Abrégé

3122 are each individually a leaving group. The method uses easily available raw materials, avoids the use of toxic and harmful reagents, is mild in terms of reaction conditions, is simple to operate, achieves a substantial improvement in yield and reduction in cost, and is more favorable for commercial production.

Classes IPC  ?

• C07D 487/04 - Systèmes condensés en ortho

Abrégé

The present disclosure provides 1) crystalline Form A of Compound la or a tautomer thereof; 2) crystalline Forms D and E of Compound lb, or a tautomer and/or hydrate thereof; and 3) co-crystalline Form C of Compound 1 and Compound lb, or a tautomer thereof, each of which is represented by the formula: (Compound 1a), (Compound 1b), (Compound 1), or a tautomer thereof. The present disclosure also provides methods for preparing crystalline Form A of Compound la. Compositions including one or more of crystalline Forms A, D, E, and C and methods of treating a disease or disorder (e.g., primary hyperoxaluria (PHI), kidney and/or bladder stones, hyperoxaluria) thereof are also provided herein. Further, the present disclosure provides processes for preparing compounds (e.g., Compound 1, Compound 1b, and formula (I) - an ester of Compound 1).

Classes IPC  ?

• C07D 249/04 - Triazoles-1, 2, 3Triazoles-1, 2, 3 hydrogénés
• A61K 31/4192 - 1,2,3-Triazoles
• A61P 13/12 - Médicaments pour le traitement des troubles du système urinaire des reins

Abrégé

The present disclosure provides 1) crystalline Form A of Compound 1a or a tautomer thereof; 2) crystalline Forms D and E of Compound 1b, or a tautomer and/or hydrate thereof; and 3) co-crystalline Form C of Compound 1 and Compound 1b, or a tautomer thereof, each of which is represented by the formula: or a tautomer thereof. The present disclosure also provides methods for preparing crystalline Form A of Compound 1a. Compositions including one or more of crystalline Forms A, D, E, and C and methods of treating a disease or disorder (e.g., primary hyperoxaluria (PH1), kidney and/or bladder stones, hyperoxaluria) thereof are also provided herein. Further, the present disclosure provides processes for preparing compounds (e.g., Compound 1, Compound 1b, and formula (I) − an ester of Compound 1).

Classes IPC  ?

• C07D 249/04 - Triazoles-1, 2, 3Triazoles-1, 2, 3 hydrogénés
• A61K 31/4192 - 1,2,3-Triazoles
• A61P 13/00 - Médicaments pour le traitement des troubles du système urinaire

Abrégé

An imine reductase mutant, including a mutation in an amino acid sequence represented by SEQ ID NO: 1. The mutation in the amino acid sequence includes V171, A172, Y230, or a combination thereof. Also provided is a method for preparing (S)-nicotine, including: under suitable conditions, catalytically reducing a substrate I to (S)-nornicotine by the imine reductase mutant, and methylating (S)-nornicotine to yield (S)-nicotine.

Classes IPC  ?

• C12N 9/06 - Oxydoréductases (1.), p. ex. luciférase agissant sur des composés contenant de l'azote comme donneurs (1.4, 1.5, 1.7)
• C12P 17/16 - Préparation de composés hétérocycliques comportant O, N, S, Se ou Te comme uniques hétéro-atomes du cycle contenant plusieurs hétérocycles

Abrégé

A method for preparing (S)-nicotine by reduction includes conducting a reduction process on an alkene compound as shown in Formula I and/or an iminium cation compound as shown in Formula II, thereby producing (S)-nicotine. The method is simple, safe, reliable, and yields both high purity and high quantities of (S)-nicotine production.

Classes IPC  ?

• C12P 17/12 - Préparation de composés hétérocycliques comportant O, N, S, Se ou Te comme uniques hétéro-atomes du cycle l'azote comme unique hétéro-atome du cycle contenant un hétérocycle à six chaînons
• C07D 401/04 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique

Abrégé

A method for using reduction to prepare (S)-nicotine, the method comprising: subjecting the enamine compound represented by formula I and/or the imine cation compound represented by formula II to a reduction reaction to obtain (S)-nicotine. As most of the strategies disclosed in the prior art for preparing (S)-nicotine require methylation to obtain (S)-nicotine, or (S)-nicotine can not be obtained by enzymatic catalysis without methylation, (S)-nicotine preparation strategies are still very limited, and a novel method for the efficient preparation of (S)-nicotine without the need to use methylation has thus been innovatively developed, namely subjecting the enamine compound represented by formula I and/or the imine cation compound represented by formula II to a reduction reaction. The present synthesis method is safe and reliable, and has simple operation and a high yield and high purity.

Classes IPC  ?

• C12P 17/16 - Préparation de composés hétérocycliques comportant O, N, S, Se ou Te comme uniques hétéro-atomes du cycle contenant plusieurs hétérocycles
• C07D 401/04 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique

Produits et services

Mixing machines; industrial marking machine; packaging machines; machines for pharmaceutical processing industry; disintegrators; rubber processing machine; machinery and equipment for glass industry (including daily glass machinery); electromechanical machines for chemical industry; handling machines, automatic [manipulators]; industrial robots; electron industry equipment; gas separation equipment; engines, other than for land vehicles; pumps [parts of machines, engines or motors]; control mechanisms for machines, engines or motors; washing apparatus; 3d printers; labellers [machines]. Computer programs, recorded; computer programs, downloadable; computer software applications, downloadable; humanoid robots with artificial intelligence for use in scientific research; downloadable mobile applications; mechanisms for coin-operated apparatus; automatic measuring device; gear measuring tool; network communication equipment; cameras [photography]; surveying apparatus and instruments; chemistry apparatus and instruments; laboratory robots; microscopes; remote control apparatus; electric installations for the remote control of industrial operations. Technological research; scientific research; scientific laboratory services; chemical research; biochemical research and analysis; biological research; bacteriological research; functional testing of equipment and instruments; product testing; industrial design; computer software design; software design and development; Information Technology [IT] consultancy; cloud computing; technical consulting in the field of artificial intelligence; research in the field of artificial intelligence; database design and development.

Produits et services

Mixing machines; industrial electromechanical marking machine; packaging machines; Machines for mixing, cleaning and stirring liquids and powders for use in the pharmaceutical industry; disintegrators for chemical processing; rubber processing machine; machinery and equipment for glass industry, namely, daily glass machinery being glass-working machines; electromechanical machines for chemical industry in the nature of organic solvent and inorganic solvent preparation machines, electromechanical; material handling machines, automatic manipulators for transporting reagents and pharmaceuticals, mainly used in laboratories and factories; industrial robots; electron industry equipment being semiconductor manufacturing machines; gas separation equipment, namely, liquid separators; engines, other than for land vehicles; pumps as parts of machines, engines or motors; control mechanisms being hydraulic controls for machines, engines or motors; washing apparatus; 3d printers; labellers being electronic label printing machines for commercial use Computer programs, recorded for use in database management; computer programs, downloadable for use in database management; computer software applications, downloadable for use as a spreadsheet; humanoid robots with artificial intelligence for use in scientific research; downloadable mobile applications using artificial intelligence for home automation; mechanisms for coin-operated apparatus; automatic measuring device, namely, fluorometers; gear measuring tool in the nature of testing equipment for measuring the temperature, pressure, position or form of workpieces in a machine tool; network communication equipment being broadband wireless equipment, namely, telecommunications base station equipment for cellular and fixed networking and communications applications; cameras; surveying apparatus and instruments; chemistry apparatus and instruments being laboratory instrument for the identification and monitoring of chemical substances and compounds used in the manufacture of pharmaceutical preparations; laboratory robots; microscopes; remote control telemetering apparatus; electric installations for the remote control of industrial operations Technological research in the field of manufacturing processes; scientific research; scientific laboratory services; chemical research; biochemical research and analysis; biological research; bacteriological research; functional testing of equipment and instruments, namely, testing the functionality of apparatus and instruments related to Pharmaceuticals; product testing; industrial design; computer software design; software design and development; Information Technology [IT] consultancy; cloud computing consultation services; technical consulting in the field of artificial intelligence software customization; research in the field of artificial intelligence; database design and development

Produits et services

Bases [chemical preparations]; salts [chemical preparations]; benzene derivatives; alkaloids; chemical additives to insecticides; chemical preparations for scientific purposes, other than for medical or veterinary use; chemical preparations for analyses in laboratories, other than for medical or veterinary purposes. Pharmaceutical preparations; chemico-pharmaceutical preparations; alkaloids for medical purposes; chemical preparations for medical purposes; tobacco-free cigarettes for medical purposes; nicotine chewing tablets for use as aids to stop smoking; nicotine patches for use as aids to stop smoking; nicotine gum for use as an aid to stop smoking; preparations for destroying noxious animals. Tobacco substitutes not for medical purpose; flavorings, other than essential oils, for use in electronic cigarettes; liquid nicotine solutions for use in electronic cigarettes; liquid nicotine alternatives for use in electronic cigarettes; liquid solutions for use in electronic cigarettes; electronic cigarettes.

Produits et services

Bases [chemical preparations]; salts [chemical preparations]; benzene derivatives; alkaloids; chemical additives to insecticides; chemical preparations for scientific purposes, other than for medical or veterinary use; chemical preparations for analyses in laboratories, other than for medical or veterinary purposes. Pharmaceutical preparations; chemico-pharmaceutical preparations; alkaloids for medical purposes; chemical preparations for medical purposes; tobacco-free cigarettes for medical purposes; nicotine chewing tablets for use as aids to stop smoking; nicotine patches for use as aids to stop smoking; nicotine gum for use as an aid to stop smoking; preparations for destroying noxious animals. Tobacco substitutes not for medical purpose; flavorings, other than essential oils, for use in electronic cigarettes; liquid nicotine solutions for use in electronic cigarettes; liquid nicotine alternatives for use in electronic cigarettes; liquid solutions for use in electronic cigarettes; electronic cigarettes.

Produits et services

Bases being chemical preparations for use in biochemical and clinical research; salts being chemical preparations in the nature of salts for industrial purposes; benzene derivatives in the nature of methyl benzene; alkaloids being alkalies; chemical additives, namely, adjuvants for use in the manufacture of insecticides; chemical preparations for scientific purposes, other than for medical or veterinary use; chemical preparations for analyses in laboratories, other than for medical or veterinary purposes Pharmaceutical preparations for use in discouraging the smoking habit; chemico-pharmaceutical preparations, namely, preparations for nervous system-related diseases; alkaloids for medical purposes, namely, Nicotinic alkaloid preparations; chemical preparations for medical purposes, namely, for treating nicotine addiction; tobacco-free cigarettes for medical purposes, namely, for smoking cessation purposes; nicotine chewing tablets for use as aids to stop smoking; nicotine patches for use as aids to stop smoking; nicotine gum for use as an aid to stop smoking; preparations for destroying noxious animals Tobacco substitutes not for medical purpose; flavorings, other than essential oils, for use in electronic cigarettes; liquid nicotine solutions for use in electronic cigarettes; liquid nicotine alternatives being electronic cigarette liquid (e-liquid) comprised of glycerin for use in electronic cigarettes; liquid solutions being electronic cigarette liquid (e-liquid) comprised of propylene glycol for use in electronic cigarettes; electronic cigarettes

Produits et services

Bases being chemical preparations for use in biochemical and clinical research; salts being chemical preparations in the nature of salts for industrial purposes; benzene derivatives in the nature of methyl benzene; alkaloids being alkalies; chemical additives, namely, adjuvants for use in the manufacture of insecticides alkaloids for medical purposes, namely, Nicotinic alkaloid preparations; tobacco-free cigarettes for medical purposes, namely, for smoking cessation purposes; nicotine chewing tablets for use as aids to stop smoking; nicotine patches for use as aids to stop smoking; nicotine gum for use as an aid to stop smoking; preparations for destroying noxious animals Tobacco substitutes not for medical purpose; flavorings, other than essential oils, for use in electronic cigarettes; liquid nicotine solutions for use in electronic cigarettes; liquid nicotine alternatives being electronic cigarette liquid (e-liquid) comprised of glycerin for use in electronic cigarettes; liquid solutions being electronic cigarette liquid (e-liquid) comprised of propylene glycol for use in electronic cigarettes; electronic cigarettes

Abrégé

Provided is a method for synthesizing (S)-nicotine, comprising: under the condition of a coenzyme circulation system, by using a coenzyme as a hydrogen donor, and by using imine reductase as a catalyst, catalyzing and reducing myosmine to (S)-nornicotine, and then subjecting (S)-nornicotine to a methylation reaction so as to obtain (S)-nicotine.

Classes IPC  ?

• C12P 17/16 - Préparation de composés hétérocycliques comportant O, N, S, Se ou Te comme uniques hétéro-atomes du cycle contenant plusieurs hétérocycles
• C07D 401/04 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique

Abrégé

Provided is a method of preparation of (1R, 3S)-3-amino-1-cyclopentanol, the method including: contacting N-acylhydroxyamine and cyclopentadiene for an asymmetric cycloaddition, to yield a first intermediate I; hydrogenating the first intermediate I to yield a second intermediate II; hydrolyzing, ammonolyzing, hydrazinolyzing, or alcoholyzing an amido bond of the second intermediate II to yield a third intermediate III; and hydrogenating the third intermediate III to yield (1R, 3S)-3-amino-1-cyclopentanol.

Classes IPC  ?

• C07C 213/08 - Préparation de composés contenant des groupes amino et hydroxy, amino et hydroxy éthérifiés ou amino et hydroxy estérifiés liés au même squelette carboné par des réactions n'impliquant pas la formation de groupes amino, de groupes hydroxy ou de groupes hydroxy éthérifiés ou estérifiés
• C07C 215/44 - Composés contenant des groupes amino et hydroxy liés au même squelette carboné ayant des groupes amino ou des groupes hydroxy liés à des atomes de carbone de cycles autres que des cycles aromatiques à six chaînons du même squelette carboné liés à des atomes de carbone du même cycle ou du même système cyclique condensé

Abrégé

A preparation method for (1R,3S)-3-amino-1-cyclopentanol and salts thereof, relating to the field of organic synthesis, wherein the (1R,3S)-3-amino-1-cyclopentanol undergoes an asymmetric cycloaddition reaction with cyclopentadiene by using a chiral source in an N-acylhydroxylamine compound as a chiral inducer, to build two chiral centers of a target product. The N-acylhydroxylamine compound can be obtained by means of a one-step ammonolysis reaction between a chiral hydroxy acid ester and hydroxylamine. The raw materials of this route are widely available, cheap and easy to get, and therefore, the costs of the raw materials can be effectively reduced. The preparation method features a reasonable route, simple operation and mild reaction conditions, and thus has high atom economy and low production costs. Moreover, said method has good stereoselectivity, and the product prepared thereby has high optical purity and stable quality, and thus is suitable for large-scale industrial production.

Classes IPC  ?

• C07C 213/00 - Préparation de composés contenant des groupes amino et hydroxy, amino et hydroxy éthérifiés ou amino et hydroxy estérifiés liés au même squelette carboné
• C07C 215/44 - Composés contenant des groupes amino et hydroxy liés au même squelette carboné ayant des groupes amino ou des groupes hydroxy liés à des atomes de carbone de cycles autres que des cycles aromatiques à six chaînons du même squelette carboné liés à des atomes de carbone du même cycle ou du même système cyclique condensé
• C07D 261/20 - Composés hétérocycliques contenant des cycles oxazole-1, 2 ou oxazole-1, 2 hydrogéné condensés avec des carbocycles ou avec des systèmes carbocycliques

Abrégé

A preparation method for (1R,3S)-3-amino-1-cyclopentanol and salts thereof, relating to the field of organic synthesis, wherein the (1R,3S)-3-amino-1-cyclopentanol undergoes an asymmetric cycloaddition reaction with cyclopentadiene by using a chiral source in an N-acylhydroxylamine compound as a chiral inducer, to build two chiral centers of a target product. The N-acylhydroxylamine compound can be obtained by means of a one-step ammonolysis reaction between a chiral hydroxy acid ester and hydroxylamine. The raw materials of this route are widely available, cheap and easy to get, and therefore, the costs of the raw materials can be effectively reduced. The preparation method features a reasonable route, simple operation and mild reaction conditions, and thus has high atom economy and low production costs. Moreover, said method has good stereoselectivity, and the product prepared thereby has high optical purity and stable quality, and thus is suitable for large-scale industrial production.

Classes IPC  ?

• C07C 213/00 - Préparation de composés contenant des groupes amino et hydroxy, amino et hydroxy éthérifiés ou amino et hydroxy estérifiés liés au même squelette carboné
• C07C 215/44 - Composés contenant des groupes amino et hydroxy liés au même squelette carboné ayant des groupes amino ou des groupes hydroxy liés à des atomes de carbone de cycles autres que des cycles aromatiques à six chaînons du même squelette carboné liés à des atomes de carbone du même cycle ou du même système cyclique condensé
• C07D 261/20 - Composés hétérocycliques contenant des cycles oxazole-1, 2 ou oxazole-1, 2 hydrogéné condensés avec des carbocycles ou avec des systèmes carbocycliques

Produits et services

chemicals for industrial purposes; pharmaceutical intermediates for use in the manufacture of pharmaceuticals; chemical preparations for scientific analyses in laboratories other than for medical or veterinary purposes; chemical preservatives for use in the production of a wide variety of chemicals