The present invention relates to pure salts of amphetamine prodrug, in particular, L-lysine-d- amphetamine (known as lisdexamfetamine) and industrial advantageous process for preparation thereof. The present invention relates to the crystalline salts of lisdexamfetamine selected from crystalline lisdexamphetamine dibesylate, crystalline hydrogen sulfate (Form-1 and Form-2). Further, the present invention relates to the preparation of crystalline salts of lisdexamfetamine and wherein salts are selected from dibesylate, hydrogen sulfate and difumarate.
A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
C07C 237/06 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
C07C 303/22 - Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of sulfonic acids or halides thereof from sulfonic acids by reactions not involving the formation of sulfo or halosulfonyl groups
A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
2.
PROCESS FOR PREPARING PURE ALLYL PROTECTED KETO DERIVATIVE
The present invention provides an industrially advantageous process for the preparation of pure allyl protected keto derivative of formula I, an intermediate of ezetimibe. by using a novel O-allyl amide derivative of formula II. wherein R is methyl or ethyl
C07D 205/08 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
3.
PROCESS FOR PREPARING PURE LH-PYRAZOLO[3,4-D] PYRIMIDINE DERIVATIVE
The present invention relates to an efficient and industrially advantageous process for the preparation of pure lH-pyrazolo[3,4-d] pyrimidine derivative. In particular the present invention provides a process for the preparation of pure 4-amino-3-(4- phenoxyphenyl)-lH-pyrazolo[3,4-d] pyrimidine, a key intermediate of ibrutinib. Particularly, the present invention provides a process for the preparation of 3-amino-4-cyano-5-(4-phenoxy phenyl)pyrazole, wherein none of the intermediates have been isolated, an important precursor for the preparation of 4-amino-3-(4-phenoxyphenyl)- lH-pyrazolo[3,4-d] pyrimidine.
C07D 473/34 - Nitrogen atom attached in position 6, e.g. adenine
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
4.
PROCESS FOR THE PREPARATION OF BENZAZEPINE-2-ONE DERIVATIVE
The present, invention relates to a cost effective, environment friendly industrially viable process for the preparation of 7,8-dimethoxy-1,3-dihydro-2H-3-benzazepine-2-one, an intermediate used in the preparation of ivabradine, without using acid chloride intermediate and condensing agent.
C07C 217/74 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton
5.
AN IMPROVED PROCESS FOR PREPARING PURE MINODRONIC ACID AND INTERMEDIATES THEREOF
The present invention relates to an industrially advantageous, cost-effective, and reproducible process for preparation of pure minodronic acid, including salts, hydrates and polymorphs thereof, by using ecofriendly process for preparation of key intermediate, in high yield and high purity.
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
The present invention provides an industrially advantageous and cost-effective process for preparation of rosuvastatin of formula I or pharmaceutically acceptable salts thereof, [Formula I should be inserted here], via novel intermediates of formulae II and III. [Formula II should be inserted here], wherein R is selected from, R1 is selected from hydrogen, straight or branched chain alkyl group preferably C1-C4; [Formula III should be inserted here]. The present invention also provides novel and efficient processes for the preparation of compounds of formulae II and III, and converting these to rosuvastatin of formula I or pharmaceutically acceptable salts thereof.
C07D 239/22 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to ring carbon atoms
C07C 69/66 - Esters of carboxylic acids having esterified carboxyl groups bound to acyclic carbon atoms and having any of the groups OH, O-metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
7.
PROCESS FOR PREPARATION OF 4,5-DIMETHOXYBENZENE DERIVATIVES AND USE IN THE SYNTHESIS OF IVABRADINE AND SALTS THEREOF
The present invention relates to an improved process for preparation of 4,5-dimethoxybenzene derivatives, which are important key intermediates in the preparation of ivabradine and salts thereof. Mainly present invention relates to an efficient and industrially advantageous process for purification of 4,5-dimethoxy benzocyclbbutane derivatives, which are important key intermediates in the preparation of ivabradine and salts thereof. Particularly, the present invention relates to a process for purification of 4,5-dimethoxy- 1-cyano-benzocyclobutane of formula I, and a process for purification of (S)-N-[(4,5-dimethoxybenzocyclobut-1-yl)-methyl]-N- (methyl)amine camphosulphonic acid salt of formula II. The present invention also relates to an efficient and industrially advantageous process for preparation of 3-(2-bromo-4,5-dimethoxybenzene)propionitrile of formula III, with high purity and high yield, wherein compound of formula III is an important precursor of 4,5-dimethoxy- 1-cyano-benzocyclobutane of formula I, a key intermediate used in the preparation of ivabradine and salts thereof.
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
C07C 217/56 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by singly-bound oxygen atoms
8.
PROCESS FOR THE PREPARATION OF SILODOSIN AND ITS GAMMA FORM
The present invention provides an improved and efficient process for the preparation silodosin of formula I and pharmaceutically acceptable salts thereof Formula I. through novel tartrate salt of cyano hydroxy intermediate of formula II. Formula II The present invention also provides an improved, industrially advantageous and novel process for preparation of pure polymorphic form gamma (γ) of silodosin, wherein residual solvents are present in specified limits as per ICH guidelines. ·
A61K 31/4045 - Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 209/08 - Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
9.
PROCESS FOR THE PREPARATION OF TAPENTADOL VIA NOVEL INTERMEDIATE
The present invention relates to a commercially viable and improved process for preparation of tapentadol of formula I and its pharmaceutically acceptable salts, Formula I via novel intermediates tertiary hydroxy protected sulfonyl compound of formula III. Formula III wherein R1 is selected from hydrogen, straight chain or branched alky I, aryl, aralkyl, alkaryl which can be substituted or unsubstituted; and R2 represents CH3-CO-, CF3-CO-, CH2CICO-, CHCI2-CO-, CCI3-CO-, CH3O-CO-CO-, CH3O-CO-, CH3CH2O-CO-, CH3CH2O-CO-CO, phenyl-CO-, or meta-CH3COO-phenyl- CO- or -S02R'; wherein R' can be selected from hydrogen, straight chain or branched alkyl, aryl, aralkyl, alkaryl, heteroalkyl, heteroaryl and like which can be substituted or unsubstituted.
A61K 31/00 - Medicinal preparations containing organic active ingredients
C07C 213/02 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
Provided is a novel polymorphic form I of rifaximin and a process for preparation thereof. The novel polymorphic form I is characterized by powder x-ray diffraction pattern at 2Θ 5.2, 7.2, 8.4 and 8.7 degrees±0.2 and water content within the range of 2.0 to 4.5%. A process for preparation of novel polymorphic form I by treating rifaximin with a mixture of ethyl alcohol and water is also provided.
C07D 498/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
11.
PROCESS FOR PREPARATION OF LISDEXAMPHETAMINE AND SALTS THEREOF
An improved, efficient, safe and convenient process for preparation of lisdexamphetamine and its pharmaceutically acceptable salts by using novel mixed anhydride intermediate is provided. A process for preparation of diamino protected amide compound namely BOC protected lisdexamphetamine, a key intermediate in the preparation of lisdexamphetamine and its pharmaceutically acceptable salts by using novel mixed anhydride intermediate and its purification by crystallization are also provided. Further, novel mixed anhydride intermediate is provided too.
C07C 237/06 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
C07C 271/22 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
C07C 269/04 - Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups from amines with formation of carbamate groups
12.
PROCESS FOR PREPARING ROSUVASTATIN CALCIUM THROUGH NOVEL AMINE SALT
The present invention provides a process for preparing pure rosuvastatin of formula (I), or pharmaceutically acceptable salts thereof through rosuvastatin l-(l-naphthyl)ethyl salt of formula (II) wherein wavy line (〰) represent (R), (S) stereochemistry or racemate thereof.
Disclosed is a process for the preparation of imatinib of formula (I), or its mesylate salt with controlled level of genotoxic impurity of formula (II), a key intermediate for imatinib.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
14.
PROCESSES FOR PREPARATION OF MONTELUKAST SODIUM AND PURIFICATION OF DIOL INTERMEDIATE
A process for preparation of montelukast sodium through novel montelukast amine salts is provided, wherein the amine is selected from 1- (l-naphthyl)ethylamine, S-methyl-L-cysteine, diallylamine or isomers thereof. A process for purification of 2-(2-(3-(S)-(3-(7-chloro-2-quinolinyl)-ethenyl)phenyl)-3-hydroxylpropyl)-phenyl-2-propanol is also provided, which uses a halogenated hydrocarbon and a nitrile as solvent.
Disclosed is a process for preparing aripiprazole polymorph hydrate A, form B and type II. Also provided is a process for preparing aripiprazole polymorph having an average particle size less than 100 μιη using a specific solvent system and reaction condition for inducing precipitation.
A process for preparation of sunitinib malate is provided, which comprises condensing an indole intermediate with formyl amide intermediate. A process for preparation of crystalline form I of sunitinib malate is also provided, which uses methyl isobutyl ketone as solvent.
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Provided is a process for the preparing l-phenyl-3-dimethylaminopropane derivatives of formula I, (The formula should be inserted here) and its pharmaceutically acceptable salts thereof via novel intermediates.
C07C 213/08 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups
C07C 215/54 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by hydroxy groups linked by carbon chains having at least three carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
C07C 217/62 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by singly-bound oxygen atoms linked by carbon chains having at least three carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
C07C 219/22 - Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings
Provided is a process for preparing androstenone derivatives, specifically 3-oxo-4-aza-5α-androstene-17β-carboxylic acid of Formula I, a key intermediate for dutasteride.
C07J 75/00 - Processes for the preparation of steroids, in general
C07J 73/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
The present invention relates to an improved and industrially advantageous process for preparation of eletriptan of formula I, or pharmaceutically acceptable salts thereof from bromo indole intermediate of formula II, through isolation of N-acetylated bromo indole intermediate of formula III, to elude carrying forward of impurities to next stage. The present invention relates to process for the preparation of 5-bromo-3-[(R)-1-methyl-pyrrolidin-2-ylmethyl]-1H-indol of formula II, a key intermediate for the synthesis of eletriptan or pharmaceutically acceptable salts thereof, through novel keto carbamate intermediate. The present invention also relates to novel process for the preparation of α-form of eletriptan hydrobromide.
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
20.
'PROCESS FOR THE PREPARATION OF COLESEVELAM HYDROCHLORIDE"
The present invention provides an industrially advantageous and efficient process for the preparation of colesevelam hydrochloride using dried colesevelam and a source of chloride ion which includes hydrogen chloride gas, solvent saturated with hydrogen chloride gas; hydrochloride salt of a suitable amine having formula NR1 R2R3. HCl (wherein R1R2 and R3 can be same or different and can be individually selected amongst hydrogen, substituted or unsubstituted alkyl or aryl or alkaryl, aralkyl, heteroaryl); sulfur compounds; carboxylic acid chloride having formula R1COCI (wherein R1 is as defined above; silyl chloride of formula R1 R2R3SiC1 (wherein R1 R2 and R3 are as defined above); metal chlorides such as TiCI4; TiCl3; BCI3; AlCl3; PCI3; PCl5; or alkali metal chloride in combination with a sulfuric acid and the like or in combination thereof.
The present invention provides an improved process for the preparation of highly pure bexarotene of formula (I). The present invention also provides impurities of bexarotene, method of isolation and identification of these impurities, and use of these impurities as reference marker as well as reference standard.
C07C 63/44 - Polycyclic acids with carboxyl groups bound to condensed ring systems containing three or more rings containing one carboxyl group
C07C 49/788 - Ketones containing a keto group bound to a six-membered aromatic ring polycyclic with keto groups bound to a condensed ring system
C07C 69/76 - Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a six-membered aromatic ring
C07C 13/38 - Polycyclic hydrocarbons or acyclic hydrocarbon derivatives thereof with condensed rings with a bicyclo ring system containing six carbon atoms
22.
ACID ADDITION SALTS OF IVABRADINE AND PREPARATION METHOD THEREOF
Provided are the novel acid addition salts of ivabradine of formula I including their hydrates, solvates, anhydrous form, and non-solvated form, all in amorphous or crystalline forms.
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
23.
PROCESS FOR PREPARING 1 -PHENYL-3 -DIMETHYLAMINOPROPANE DERIVATIVES
Process for preparing 1-phenyl-3-dimethylaminopropane derivatives of formula (I), and pharmaceutically acceptable salts thereof from intermediate of formula (II) are provided, wherein R1 can be selected from -OR2, halo, -CH2OR2, -SR2, SOR2, SO2R2, -SO3H, -NO2, -NR2R2', - CONR2R2 ', and the like; R ' can be selected from hydrogen, alkyl, aryl, aralkyl, alkaryl, heteroaryl, and the like; or R2 and R2 ' can be same or different and can be selected from hydrogen, alkyl, aryl, aralkyl, heteroaryl,-OR3, - COR3, -PO3(R3R1) wherein R1 and R4 can be same or different and can be selected from alkyl, aryl, aralkyl, heteroaryl and the like.
C07C 215/54 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by hydroxy groups linked by carbon chains having at least three carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
C07C 213/00 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
C07C 217/62 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by singly-bound oxygen atoms linked by carbon chains having at least three carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
C07C 211/27 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring having amino groups linked to the six-membered aromatic ring by saturated carbon chains
24.
PROCESS FOR THE PREPARATION OF 1-PHENYL-3-DIMETHYLAMINOPROPANE DERIVATIVES
A process for the preparation of 1-phenyl-3-dimethylaminopropane derivatives of formula (I) and its pharmaceutically acceptable salts thereof from cyano intermediate of formula (II), wherein R1 can be selected from -OR2, halo, -CH2OR2, -SR2, -SOR2, SO2R2, -SO3H, -NO2, -NR2R2', -CONR2R2', carboxylic esters, sulfonate esters or phosphate esters, R2 and R2' can be same or different, and can be selected from hydrogen, alkyl, aryl, aralkyl, heteroaryl, -COR2", -P03(R2")2 wherein R2" can be selected from alkyl, aryl, aralkyl, heteroaryl and the like.
C07D 213/02 - Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
C07D 215/42 - Nitrogen atoms attached in position 4
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 233/90 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07C 225/06 - Compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly-bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being saturated and acyclic
The present invention provides an improved, industrial advantageous process for the preparation of gefitinib of formula (I), and its pharmaceutically acceptable salts thereof in high yield and purity.
The present invention relates to an efficient and cost-effective process for the preparation of 6- methylenandrost-1,4-diene-3,17-dione (exemestane) by dehydrogenation of 6-methylenandrost-4- ene-3,17-dione using an dehydrogenating agent in the presence of an acid catalyst and at least one co-oxidant in an organic solvent.
C07J 1/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, not substituted in position 17 beta by a carbon atom, e.g. oestrane, androstane
A process for the preparation of (S)-pregabalin of formula I containing cyanide ion content less than 5 ppm or free from the cyanide ion,by extracting its cyano diester intermediate of formula III, wherein R1 and R2 are the same or different and are hydrogen, C1-C6 alkyl, aryl, benzyl, substituted benzyl, or C3-C6 cycloalkyl. with an aqueous solution containing a cyanide quenching agent to remove free cyanide ion from the reaction mixture.
C07C 253/00 - Preparation of carboxylic acid nitriles
C07C 229/08 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to hydrogen atoms
30.
PROCESS FOR PREPARING CINACALCET AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
The resent invention rovides a novel rocess for re arin cinacalcet of formula I and pharmaceutically acceptable salts thereof and process of purification. The present invention also provides novel nitrogen protected synthetic intermediates useful in the process of the present invention. Further, the present invention provides a novel substituted carbamate impurity and process of preparation thereof.
C07C 211/30 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring the six-membered aromatic ring being part of a condensed ring system formed by two rings
The present invention provides a process for the preparation of indole derivatives, specifically N- methyl-1H-indole-5-ethanesulfonamide of formula (I), involving novel intermediate, which is used as key intermediate for the synthesis of naratriptan of formula (II), and its pharmaceutically acceptable salts thereof high yield and purity.
C07D 209/08 - Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07C 311/35 - Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atoms of the sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings
C07D 209/30 - Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
32.
PROCESS FOR PREPARING EZETIMIBE USING NOVEL ALLYL INTERMEDIATES
The present invention provides an efficient and industrially advantageous process for the preparation of ezetimibe of formula (I), using novel intermediates.
C07D 205/08 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
C07D 263/26 - Oxygen atoms attached in position 2 with hetero atoms or acyl radicals directly attached to the ring nitrogen atom
C07C 251/24 - Compounds containing nitrogen atoms doubly- bound to a carbon skeleton containing imino groups having carbon atoms of imino groups bound to carbon atoms of six-membered aromatic rings
C07C 403/12 - Derivatives of cyclohexane or of a cyclohexene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene rings, e.g. vitamin A, beta-carotene, beta-i having side-chains substituted by singly-bound oxygen atoms by esterified hydroxy groups
33.
AN IMPROVED PROCESS FOR SYNTHESIZING HIGHLY PURE ATOMOXETINE
The present invention relates to a process for the preparation of highly pure atomoxetine of formula (I) and pharmaceutically acceptable salts thereof Formula (I) The present invention also aims at novel processes for the preparation and purification of intermediates involved in the process of the present invention.
C07C 213/06 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton from hydroxy amines by reactions involving the etherification or esterification of hydroxy groups
C07C 213/02 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
34.
PROCESS FOR PREPARING POSACONAZOLE AND INTERMEDIATES THEREOF
The present invention relates to an industrially advantageous process for the preparation of tetrahydrofuran antifungals preferably posaconazole of formula I. The present invention further relates to improved processes for preparing key and novel intermediates useful in the preparation of posaconazole. The present invention further relates to improved processes for preparing the compound of formula II, a key intermediate in the preparation of posaconazole.
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
35.
PROCESS FOR THE PREPARATION OF HIGHLY PURE PRULIFLOXACIN
The present invention provides an industrially advantageous process for the preparation of highly pure prulifloxacin of formula I and its pharmaceutically acceptable salts. The present i innvention a also provides a novel process for the purification of prulifloxacin acid addition salt.
The present invention relates to an industrially advantageous process for the preparation of O- desmethyl-venlafaxine, a venlafaxine metabolite, and pharmaceutically acceptable salts thereof by demethylating venlafaxine or salts using an alkali or alkaline earth metal salts of mercapto acids and their derivatives, mercapto alcohols, heterocyclic mercaptans, xanthates and thioacids and the like or mixture thereof in presence of an organic solvent.
C07C 209/68 - Preparation of compounds containing amino groups bound to a carbon skeleton from amines, by reactions not involving amino groups, e.g. reduction of unsaturated amines, aromatisation, or substitution of the carbon skeleton
C07C 213/00 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
C07C 215/52 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by hydroxy groups linked by carbon chains having two carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
37.
PROCESS FOR THE PREPARATION OF PERHYDROISOINDOLE DERIVATIVE
The present invention relates to a novel, efficient and industrially advantageous process for preparing perhydroisoindole derivative, particularly (S)-mitiglinide of formula (I): and pharmaceutically acceptable salts thereof. Further, it relates to novel amide intermediates of formula (VI), including salts, solvates, hydrates, polymorphs, isomers and racemic mixtures thereof useful in the process of present invention. Formula (VI): wherein R is selected from straight chain or branched C1-6 alkyl, unsubstituted or substituted aryl, unsubstituted or substituted arylalkyl. The present invention also relates to amorphous form of mitiglinide calcium, its preparation and process for its conversion to crystalline mitiglinide calcium.
C07D 263/26 - Oxygen atoms attached in position 2 with hetero atoms or acyl radicals directly attached to the ring nitrogen atom
C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
38.
PROCESS FOR THE PREPARATION OF AMORPHOUS FEXOFENADINE HYDROCHLORIDE
The present invention provides a process for the preparation of amorphous fexofenadine hydrochloride from fexofenadine via its weak acid addition salt, in high yield and purity. The present invention further provides a process for the preparation of amorphous fexofenadine hydrochloride from fexofenadine acid addition salt.
C07D 211/22 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms by oxygen atoms
39.
PROCESS FOR THE PREPARATION OF 3-ARYLOXY-3-ARYLPROPANAMINES
The present invention provides a process for the preparation of 3-aryloxy-3-arylρropanamine derivatives. Particularly the present invention provides a process for the preparation of duloxetine and pharmaceutically acid addition salts thereof specifically, duloxetine hydrochloride of formula (I), using 3-O-protected propanolamine derivatives. The invention also aims at providing a process for the preparation of highly pure duloxetine hydrochloride of formula (I) from duloxetine free base via its acid addition salts The invention further aims at providing a process for the purification of duloxetine hydrochloride, wherein the level of unwanted R-enantiomer is reduced to nearly 0%.
C07D 333/04 - Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulfur atom
40.
PURIFICATION PROCESS TO PREPARE HIGHLY PURE ANASTROZOLE
The present invention relates to an industrially advantageous method for the purification of anastrozole of Formula (I), wherein isoanastrozole of Formula (VI), present in crude anastrozole as an impurity, is removed by using gel purification.
C07C 255/35 - Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by halogen atoms, or by nitro or nitroso groups
41.
PROCESS FOR THE PREPARATION OF IVABRADINE HYDROCHLORIDE AND POLYMORPH THEREOF
The present invention encompasses a process for the preparation of highly pure ivabradine hydrochloride by treating ivabradine with alcoholic hydrogen chloride. The invention further encompasses amorphous ivabradine hydrochloride and process for its preparation using suitable acid addition salts of ivabradine.
The present invention relates to an industrially advantageous process for the preparation of ezetimibe of formula (I) in high yields by using novel benzyl ester intermediates. The present invention further provides a process for the purification of ezetimibe of formula (I).
C07D 205/08 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
C07D 263/26 - Oxygen atoms attached in position 2 with hetero atoms or acyl radicals directly attached to the ring nitrogen atom
43.
PROCESS FOR SYNTHESIZING HIGHLY PURE NATEGLINIDE POLYMORPHS
The present invention relates to an improved process for synthesizing highly pure nateglinide of formula-(I). More particularly, the present invention relates to the process for synthesizing highly enantiomerically pure nateglinide form B and form H directly from nateglinide alkyl ester.
C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
C07C 231/08 - Preparation of carboxylic acid amides from amides by reaction at nitrogen atoms of carboxamide groups
C07C 231/22 - Separation; Purification; Stabilisation; Use of additives
C07C 233/46 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
44.
AN INDUSTRIAL PROCESS FOR THE PREPARATION OF PURE ROPINIROLE
The present invention relates to highly pure ropinirole or salt thereof and a process for preparing highly pure ropinirole of structural formula (I): by reducing nitro compound of formula (II): with a hydrogen gas in the presence of a catalyst in water to produce amino compound and cyclizing the resulting amino compound in situ.
The present invention relates to an industrially advantageous process for the preparation of thiazolidine derivatives, such as pioglitazone of formula I and its pharmaceutically acceptable salts.This invention also provides novel synthetic intermediates useful in the process for the preparation of pioglitazone.
C07D 417/00 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group
The present invention relates to a novel process for the preparation of indole derivatives. In particular, present invention relates to the process for preparing naratriptan of formula (I), and its salts using novel intermediates. The present invention also relates to novel synthetic intermediates useful in the preparation of naratriptan hydrochloride.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
The present invention relates to an industrially advantageous, eco-friendly process for the re aration of rimonabant of formula-(I), staring from l-(4-chlorophenyl)-propan-l-one in high yields and high purity by using mild reaction conditions and avoiding use of toxic and expensive reagents, as well as stringent reaction conditions. The present invention relates to an isolated impurity of rimonabant, referred to as 'Bis impurity' and removal thereof.1 The present invention also relates to novel crystalline form-Ill of rimonabant and processes for its preparation and conversion to form-I of rimonabant.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/00 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
48.
IMPROVED PROCESS FOR THE PREPARATION OF RANOLAZINE
The present invention provides an improved process for the preparation of ranolazine of formula I and pharmaceutically acceptable salts thereof, by reacting 2,6-dimethylaniline derivative with chloroacetyl chloride in the presence of base in water and resulting amide intermediate is reacted with piperazine and the resulting piperazinc derivative is further condensed with an appropriate oxirane derivative ( prepared by the reaction of 2-methoxyphenol with epichlorohydrin in the presence of base using phase transfer catalyst) in an inert solvent, and highly pure ranolazine is isolated and converted to its acid salts using excess of mineral acid.
C07D 233/02 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
49.
PROCESS FOR THE PREPARATION OF AMINE DERIVATIVES AS CALCIMIMETICS
The present invention relates to a novel process for preparing amine derivatives of formula (I), and pharmaceutically acceptable salts and complexes thereof, wherein Ar1or Ar2 is either naphthyl or phenyl optionally substituted with 0 to 5 subslituents each independently selected from the group consisting of lower alkyl, halogen, lower alkoxy, lower thioalkyl, methylene dioxy, lower haloalkyl, lower haloalkoxy, OH, CH2OH, CONH2, CN, acetoxy; q is 0-2; and R is H, by reducing novel amide intermediates of formula (II) wherein Ar1, Ar2 and q are same as described above. Particularly the present invention relates to an industrially advantageous process for the preparation of cinacalcet hydrochloride of formula (III) using novel amide intermediate of formula (VIII), wherein X is H, halo like chloro, bromo or iodo.
The present invention relates to process for preparing antihistaminic piperidine derivative, specifically fexofenadine and its pharmaceutically acceptable salts by using novel synthetic intermediates of following formula (I), wherein R is lower alkyl; R2 is H, cyclopropyl, R1 is alkyl, 4-(hydroxy-diphe&tgr;iyl-methyl)-piperidin-l-yl.
C07D 211/00 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
C07D 211/22 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms by oxygen atoms
51.
PROCESS FOR THE PREPARATION OF PURE RISEDRONIC ACID OR SALTS
The present invention relates to an industrially advantageous process of making bisphosphonic acid or its salt in particular risedronic acid, ⏧l-hydroxy-2(3-pyridinyl)ethylidene] bisphosphonic acid, having formula-(I) or its salts in high purity and high yields.
C07D 213/04 - Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
52.
PROCESS FOR THE PREPARATION OF POLYMORPHIC FORMS OF CLOPIDOGREL HYDROGEN SULFATE
The present invention relates to a novel process for the preparation of polymorphic forms of clopidogrel hydrogen sulfate, namely methyl (+)-(S)-α-(o-chlorophenyl)-6,7-dihydrotliieno [3,2-c] pyridine-5(4H)-acetate hydrogen sulfate of formula (I). Particularly the present invention relates to the process for the preparation of form (I) and amorphous clopidogrel hydrogen sulfate.
C07D 513/02 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups , or in which the condensed system contains two hetero rings
53.
A PROCESS FOR THE PREPARATION OF HIGHLY PURE ANHYDROUS FEXOFENADINE HYDROCHLORIDE
The present invention relates to a novel and industrially advantageous process for the preparation of highly pure anhydrous Fexofenadine hydrochloride directly from fexofenadine base without isolating hydrous Fexofenadine hydrochloride.
C07D 211/22 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms by oxygen atoms
54.
PROCESS FOR THE PREPARATION OF HIGHLY PURE DONEPEZIL
The present invention relates to the preparation of highly pure donepezil of formula I or salt thereof, by hydrogenating indanonylidenyl compound of formula II, using platinum catalysts.
C07D 211/32 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom by oxygen atoms
C07D 211/14 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
C07D 211/16 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with acylated ring nitrogen atom
C07D 211/20 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms
C07D 211/22 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms by oxygen atoms
C07C 43/168 - Unsaturated ethers containing six-membered aromatic rings containing six-membered aromatic rings and other rings
C07C 49/563 - Unsaturated compounds containing keto groups bound to rings other than six-membered aromatic rings containing six-membered aromatic rings
C07C 49/395 - Saturated compounds containing a keto group being part of a ring of a five-membered ring
C07C 49/427 - Saturated compounds containing a keto group being part of a ring polycyclic a keto group being part of a condensed ring system having two rings
C07C 49/443 - Saturated compounds containing a keto group being part of a ring polycyclic a keto group being part of a condensed ring system having two rings the condensed ring system containing eight or nine carbon atoms
55.
AN IMPROVED PROCESS FOR THE PREPARATION OF PURE VENLAFAXINE
The present invention relates to pure Venlafaxine or salt thereof and a process for preparing highly pure Venlafaxine of structural Formula (I), Formula (I) from N, N-didesmethyl venlafaxine or salt thereof of formula (III).
C07C 211/27 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring having amino groups linked to the six-membered aromatic ring by saturated carbon chains
56.
AN IMPROVED PROCESS FOR THE PREPARATION OF HIGHLY PURE FEXOFENADINE
The present invention provides an improved process for the preparation of highly pure 4-⏧1-hydroxy-4-⏧4-(hydroxydiphenylmethyl)-1-piperidinyl]-butyl]-&agr;,&agr;-dimethylbenzene acetic acid (fexofenadine) of Formula (I), or its salts thereof.
C07D 211/22 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms by oxygen atoms
57.
A PROCESS FOR THE PREPARATION OF 6-O-METHYL ERYTHROMYCIN A DERIVATIVE
The present invention relates to an improved process for the preparation of 6-O-methylerythromycin A derivatives, intermediates of clarithromycin, by selective methylation of erythromycin A derivative in a mixture of a acyclic or cyclic alkanes having C6-C10 carbon atoms, and a polar aprotic solvent using a methylating agent in the presence of a base under mild conditions.
patents