C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
C07C 215/10 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic with one amino group and at least two hydroxy groups bound to the carbon skeleton
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
2.
GARENOXACIN MESYLATE, PROCESS FOR PREPARATION THEREOF, AND CRYSTALLINE FORM THEREOF.
Provided are garenoxacin mesylate, process for preparation thereof, and crystalline form thereof. The garenoxacin mesylate crystalline form is characterized by an X-ray powder diffraction pattern with peaks at about 13.77, 20.54, 21.50, 21.77, 22.12 and 23.90±0.20. A pharmaceutical composition of the garenoxacin mesylate crystalline form is also provided.
C07D 215/56 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4
The present invention provides a process for preparation of fingolimod, a compound of Formula I or a pharmaceutically acceptable salt thereof, free of regioisomeric impurity compound of Formula IA
C07C 205/16 - Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by hydroxy groups having nitro groups and hydroxy groups bound to acyclic carbon atoms of a carbon skeleton containing six-membered aromatic rings
C07C 209/34 - Preparation of compounds containing amino groups bound to a carbon skeleton by reduction of nitrogen-to-oxygen or nitrogen-to-nitrogen bonds by reduction of nitro groups by reduction of nitro groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
C07C 209/70 - 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 by reduction of unsaturated amines
C07C 215/28 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having 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
4.
PROCESS FOR PREPARATION OF 2-ACETAMIDO-N-BENZYL-3-METHOXYPROPIONAMIDE
C07C 237/22 - 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 having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
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 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
C07C 231/20 - Preparation of optical isomers by separation of optical isomers
The present invention provides a process for the preparation of substituted 3'-hydrazino-biphenyl-3-carboxylic acid compounds. The present invention further provides a process for the preparation of 3'-{N'-[1-(3,4-dimethylphenyl)-3-methyl-5-oxo-1,5-dihydro-pyrazol-4-ylidene]hydrazino}-2'-hydroxybiphenyl-3-carboxylic acid, its intermediate compounds and pharmaceutically acceptable salts thereof.
C07D 231/08 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with oxygen or sulfur atoms directly attached to ring carbon atoms
C07C 251/12 - Compounds containing nitrogen atoms doubly- bound to a carbon skeleton containing imino groups having carbon atoms of imino groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of an unsaturated carbon skeleton being acyclic
6.
A PROCESS FOR THE PREPARATION OF AMORPHOUS ROSUVASTATIN CALCIUM
The present invention provides a process for the preparation of paliperidone palmitate comprising reacting paliperidone with palmitic acid or its derivative in the presence of a mixture of an organic base and an inorganic base.
The present invention provides a process for purification of diacerein, compound of Formula I, the process comprising a. reacting diacerein, compound of Formula I with a silylating agent to form a compound of Formula II, silylated diacerein wherein R is alkyl; and [Formula (I)] [Formula (II)] b. deprotecting compound of Formula II, silylated diacerein in presence of a polar solvent.
Disclosed are a process for the preparation of (S)-(+)-10,ll-dihydro-10-hydroxy-5H-dibenz[b,f]azepine-5-carboxamide (eslicarbazepine), (S)-(-)-10-(acetyloxy)-10,ll-dihydro-5H-dibenz[b,f]azepine-5-carboxamide (eslicarbazepine acetate) and novel compounds that may be useful intermediates in the preparation thereof.
C07D 223/28 - Dibenz [b, f] azepinesHydrogenated dibenz [b, f] azepines with hydrocarbon radicals, substituted by nitrogen atoms, attached to the ring nitrogen atom having a single bond between positions 10 and 11
10.
PROCESS FOR PREPARATION OF PRASUGREL AND ITS INTERMEDIATES
C07C 45/63 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by introduction of halogenPreparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by substitution of halogen atoms by other halogen atoms
C07C 49/567 - Unsaturated compounds containing keto groups bound to rings other than six-membered aromatic rings containing halogen
C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
C07C 205/43 - Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by esterified hydroxy groups having nitro groups or esterified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton to carbon atoms of the same non-condensed six-membered aromatic ring or to carbon atoms of six-membered aromatic rings being part of the same condensed ring system
12.
UNSOLVATED FORM OF RANELIC ACID AND PROCESS FOR PREPARATION THEREOF
Provided is preparation method of R-sitagliptin. Compound of formula (IV), amine salt thereof and method for preparation thereof are also provided. Said compound of formula (IV) or amine salt thereof is useful as key intermediate in the synthesis of R-sitagliptin or pharmaceutically acceptable salts thereof.
Disclosed is a process for preparing dronedarone and pharmaceutically acceptable salts thereof. Also disclosed are a novel amorphous form of dronedarone hydrochloride and a preparation process thereof.
C07D 307/80 - Radicals substituted by oxygen atoms
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
C07D 307/79 - Benzo [b] furansHydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
15.
PROCESS FOR PREPARATION OF MILNACIPRAN INTERMEDIATE AND ITS USE IN PREPARATION OF PURE MILNACIPRAN
C07D 209/48 - Iso-indolesHydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
C07D 307/93 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems condensed with a ring other than six-membered
C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
C07C 237/24 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
16.
PROCESS FOR PREPARATION OF POSACONAZOLE AND CRYSTALLINE POLYMORPHIC FORM V 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
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
Disclosed is a process for the preparation of 2,3-diaryl-5-substituted pyridines (compounds of formula I). Also, novel compounds of formula II and a process for the preparation thereof are disclosed.
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 211/78 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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
19.
RASAGILINE SALTS AND PROCESSES FOR THE PREPARATION THEREOF
The present invention relates to crystalline salts of rasagiline and processes for the preparation thereof. The invention also relates to pharmaceutical compositions comprising the same.
C07C 211/42 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of an unsaturated carbon skeleton containing condensed ring systems with six-membered aromatic rings being part of the condensed ring systems
C07C 209/82 - PurificationSeparationStabilisationUse of additives
A process for preparation of propargylated aminoindans or pharmaceutically acceptable salts thereof, comprises: a) reacting an indanone derivative or a salt thereof with propargyl amine or a salt thereof in the presence of a Lewis acid; b) subjecting the resultant reaction mixture to reduction.
C07C 211/42 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of an unsaturated carbon skeleton containing condensed ring systems with six-membered aromatic rings being part of the condensed ring systems
C07C 209/22 - Preparation of compounds containing amino groups bound to a carbon skeleton by substitution of functional groups by amino groups by substitution of other functional groups
C07C 271/44 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
C07C 269/06 - 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 by reactions not involving the formation of carbamate groups
A61K 31/135 - Amines, e.g. amantadine having aromatic rings, e.g. methadone
A crystalline form of prasugrel hydrobromide, the preparation method and application thereof are provided. The crystalline prasugrel hydrobromide is prepared by precipitation of prasugrel with hydrobromic acid in solvents. The prasugrel hydrobromide can be converted into prasugrel hydrochloride or used as a component of a pharmaceutical composition.
A61K 31/4365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
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
A solid crystalline form of 1-(2-[4-(6-methoxy-3, 4-dihydronaphthalene-1-y) phenoxy]ethyl) pyrrolidine, and a preparing process thereof are provided. The aforesaid compound is a key intermediate in the synthesis of lasofoxifene. A process for preparing lasofoxifene, a process for purifying lasofoxifene tartrate, and a crystalline form of lasofoxifene tartrate are also provided.
C07D 207/08 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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 radicals, substituted by hetero atoms, attached to ring carbon atoms
C07D 295/088 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
A process for purifying eslicarbazepine acetate is provided The crystalline particles of eslicarbazepine acetate having a median particle size between 5 μm and 20 μm and a specific surface area of from 0.1 m2/g to 10 m2/g as measured by B.E.T. method are obtained Eslicarbazepine acetate having purity greater than 99.0% as measured by high performance liquid chromatography and a pharmaceutical composition containing the same are also provided.
C07D 223/28 - Dibenz [b, f] azepinesHydrogenated dibenz [b, f] azepines with hydrocarbon radicals, substituted by nitrogen atoms, attached to the ring nitrogen atom having a single bond between positions 10 and 11
C07D 223/24 - Dibenz [b, f] azepinesHydrogenated dibenz [b, f] azepines with hydrocarbon radicals, substituted by nitrogen atoms, attached to the ring nitrogen atom
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
The present invention provides a process for preparation of racemic voriconazole in a single reaction vessel. The present invention also provides a process for preparation of voriconazole using racemic voriconazole and the process of making it therewith.
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
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
26.
A PROCESS FOR THE PREPARATION OF ZOFENOPRIL AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
The present invention relates to a process for the preparation of zofenopril and its pharmaceutically acceptable salts and a pharmaceutical composition thereof. The present invention also provides structurally novel compounds, which are useful intermediates in the synthesis of zofenopril.
The present invention relates to processes for the preparation of prasugrel and its pharmaceutically acceptable salts, including novel crystalline forms of prasugrel hydrochloride, and pharmaceutical compositions thereof. The present invention also relates to solid state properties of prasugrel or a pharmaceutically acceptable salt thereof.
The present invention relates to an improved process for the synthesis of strontium ranelate or hydrates thereof. More particularly, the present invention relates to an effective process for the preparation of a compound of formula (III), which is a useful intermediate in the synthesis of strontium ranelate wherein R1 and R2 represents substituted or unsubstituted linear or branched C1-C6 alkyl group or C3-C12 cyclic group.
The present invention generally relates to a process for the preparation of fosaprepitant dimeglumine intermediate and its use in the preparation of fosaprepitant dimeglumine; to a neutral form of fosaprepitant in a solid state and processes for the preparation thereof; and to a stable amorphous fosaprepitant dimeglumine, having a stability at temperatures of about 2°C to about 8°C and at a relative humidity below at least 60%; and a process for the preparation thereof.
The present invention provides an amorphous bupropion hydrobromide and an amorphous bupropion hydrobromide granulates with at least one pharmaceutically acceptable carrier, and a process for its preparation.
C07C 225/16 - 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 unsaturated and containing six-membered aromatic rings
C07C 221/00 - Preparation of compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton
A61K 31/135 - Amines, e.g. amantadine having aromatic rings, e.g. methadone
31.
A PROCESS FOR THE PREPARATION OF PALIPERIDONE INTERMEDIATES
The present invention relates to a process for the preparation of 3-(2-chloroethyl)-6, 7, 8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[1,2-a]-pyrimidin-4-one; and its use in the synthesis of paliperidone.
The present invention provides novel palonosetron free base in an amorphous form and crystalline form-G and processes for their preparation. The present invention also provides a process for the preparation of palonosetron hydrochloride from the novel palonosetron free base in an amorphous form and/or in crystalline form-G.
C07D 453/02 - Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
33.
A PROCESS FOR THE PREPARATION OF R-SIT AGLIPTIN AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
The present invention provides ramelteon substantially in an amorphous form and a process for its preparation, by preparing solution of ramelteon by dissolving in one or more solvents capable of dissolving the ramelteon; and substantially removing the solvent from the solution to provide amorphous ramelteon
C07D 307/77 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
35.
A PROCESS FOR THE SYNTHESIS OF 2-[2-[4-[(4-CHLOROPHENYL)PHENYL METHYL]-1-PIPERAZINYL] ETHOXY ACETIC ACID
TAbstract A process for the preparation of 2-[2-[4-[(4-chloro phenyl) phenyl methyl]-1-piperazinyl] ethoxy acetic acid of formula (Ia) and pharmaceutically acceptable salts thereof, and compounds of formula (IIa) and (VIIIa), wherein R1 = H or C1-C4 alkyl; R2 = aryl or heteroaryl or R1 and R2 together with the carbon to which they are attached form a C3-C8 cycloalkyl group and X is a suitable leaving group for example, chlorine, bromine, iodine, 4-methylphenyl-sulfonyloxy, methylsulfonyloxy group or 4-bromophenyl-sulfonyloxy group are described.
C07D 295/14 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07C 235/06 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same 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
36.
EPIMERIZATION BY STEREOSELECTIVE SYNTHESIS OF VITAMIN D ANALOGUES
A method for epimerization process of C-24 ketones to desired C-24 alcohol by stereo selective reduction using chiral borane reducing agents in the presence of chiral auxiliary such as (R)-2-methyl-CBS-oxazaborolidine for the preparation of calcipotriene intermediates and its process to calcipotriene.
C07C 29/143 - Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring by reduction of an oxygen-containing functional group of C=O containing groups, e.g. —COOH of ketones
C07C 35/21 - Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a ring other than a six-membered aromatic ring polycyclic, at least one hydroxy group bound to a non-condensed ring
patents