- Method for synthesizing sitagliptin and intermediate thereof through biological catalysis
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The invention provides a method for synthesizing sitagliptin and an intermediate thereof through biological catalysis, and particularly provides compounds as shown in formula I and a formula II, or pharmaceutically acceptable salt thereof, polypeptide capable of synthesizing a compound as shown in the formula I to produce a compound as shown in the formula II, nucleic acid coding the polypeptide,and a vector and a cell containing the nucleic acid. In addition, the invention further provides a method for producing the compound as shown in the formula II and sitagliptin through the polypeptideand the compound as shown in the formula I, and a preparation method for preparing the polypeptide.
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Paragraph 0145; 0147; 0148; 0149; 0150; 0152
(2018/10/11)
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- Preparation method of evogliptin
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The invention relates to the field of organic chemical synthesis and in particular to a preparation method of evogliptin. Compared with an existing production line, the preparation method of evogliptin has the characteristics of being mild in reaction con
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Paragraph 0059; 0060
(2017/07/22)
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- TETRAHYDRO-IMIDAZO[1,5-A]PYRAZINE DERIVATIVES SALTS, PREPARATION PROCESS AND PHARMACEUTICAL USE THEREOF
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The present invention relates to (R)-7-[3-Amino-4-(2,4,5-trifluoro-phenyl)-butyryl]-3-trifluoromethyl-5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine-1-carboxylic acid pharmaceutical salts, methods for their preparation, pharmaceutical compositions containing the same and their use as a therapeutic agent, especially as a dipeptidyl peptidase IV inhibitor.
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Page/Page column 14; 15; 16
(2016/10/08)
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- Chiral Lewis Base-Catalyzed, Enantioselective Reduction of Unprotected β-Enamino Esters with Trichlorosilane
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Catalytic asymmetric reduction of N-unsubstituted β-enamino esters represents a major challenge for asymmetric catalysis. In this paper, the first organocatalytic system that could be used for the asymmetric hydrosilylation of N-unsubstituted β-enamino esters has been developed. Using N-tert-butylsulfinyl-L-proline-derived amides and L-pipecolinic acid-derived formamides as catalyst, a broad range of β-aryl- and β-alkyl-substituted free β-amino esters could be prepared with high yields and enantioselectivities. The practicality was illustrated by the gram-scale asymmetric synthesis of ethyl (R)-3-amino-3-phenylpropanoate and isopropyl (S)-3-amino-4-(2,3,5-trifluorophenyl)butanoate. The resulting product can be smoothly transformed to the FDA approved medicines dapoxetine and sitagliptin in a short synthetic route.
- Ye, Jianheng,Wang, Chao,Chen, Lin,Wu, Xinjun,Zhou, Li,Sun, Jian
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supporting information
p. 1042 - 1047
(2016/04/19)
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- SALTS OF TETRAHYDROIMIDAZO Y1,5-A¨PYRAZINE DERIVATIVES, PREPARATION METHODS AND PHARMACEUTICAL USE THEREOF
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Pharmaceutical salts of (R)-7-[3-amino-4-(2,4,5-trifluorophenyl)-butyryl]-3-trifluoromethyl-5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine-1-formic acid, their preparation methods, compositions containing the said pharmaceutical salts and their use as medicaments, especially as dipeptidyl peptidase IV (DPP-IV) inhibitors are disclosed.
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Page/Page column 7-8
(2012/02/04)
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- TETRAHYDRO-IMIDAZO[1,5-a]PYRAZINE DERIVATIVES SALTS, PREPARATION METHODS AND MEDICINAL USE THEREOF
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Pharmaceutically acceptable salts of (R)-7-[3-amino-4-(2,4,5-trifluorophenyl)-butyryl]-3-trifluoromethyl-5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine-1-formic acid, their preparation methods, compositions containing the said pharmaceutical salts and their use as medicaments, especially as dipeptidyl peptidase IV (DPP-IV) inhibitors are disclosed.
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Page/Page column 8
(2012/03/27)
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- A PROCESS FOR PREPARING R-BETA-AMINO PHENYLBUTYRIC ACID DERIVATIVES
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Disclosed is a process for preparing chiral pharmaceutical intermediates of R-beta-amino phenylbutyric acid derivatives (I) and pharmaceutically acceptable salts thereof, which affords the desired object compounds having special optical configuration by chemosynthesis process comprising resolving the optical isomer mixtures of beta-amino phenylbutyric acid derivatives with resolving agent. This process comprises the resolving step of salification in alcoholic solvent or aquesous solution of alcohol with resolving agent of di-para-toluoyl-L-tartaric acid and di-para-toluoyl-D-tartaric acid. The obtained R-beta-amino phenylbutyric acid derivatives (I) have high optical purity, and the total yield of the accumulative resolution of the laevo and the dextro isomer is up to above 70%. The R-beta-amino phenylbutyric acid derivatives (I) produced by this process can be better used in synthesizing medicament.
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Page/Page column 5
(2011/04/25)
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- PROCESS FOR PREPARING R-BETA-AMINO PHENYLBUTYRIC ACID DERIVATIVES
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Disclosed is a process for preparing single enantiomers of beta-amino phenylbutyric acid derivatives and pharmaceutically acceptable salts thereof, which affords the desired compounds having special optical configuration. The process comprises a step of chemical synthesis and a step of resolving the optical isomers of beta-amino phenylbutyric acid derivatives with a resolving agent. The resolving step comprises reacting the optical isomers with resolving agents, such as di-para-toluoyl-L-tartaric acid and di-para-toluoyl-D-tartaric acid. The obtained R-beta-amino phenylbutyric acid derivatives (I) have high optical purity, and the total yield of the accumulative resolution of the laevo and the dextro isomer is up to above 70%.
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Page/Page column 3-4
(2011/06/23)
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- PROCESS FOR THE PREPARATION OF SITAGLIPTIN AND ITS INTERMEDIATES
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The present invention relates to novel and improved processes for the preparation of Sitagliptin compound of formula (1) and its intermediates.
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Page/Page column 43-44
(2010/11/05)
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- TETRAHYDRO-IMIDAZOY1,5-A¨PYRAZINE DERIVATIVES, PREPARATION METHODS AND MEDICAL USES THEREOF
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Tetrahydro-imidazo[1,5-a]pyrazine derivatives of formula ( I ), their preparation methods, pharmaceutical compositions containing the derivatives and uses thereof as medicaments, especially as dipeptidyl peptidase IV inhibitor, wherein the substituents of formula ( I ) are defined as same as the description.
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Page/Page column 17
(2010/10/03)
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- TARTARIC ACID SALTS OF A DIPEPTIDYL PEPTIDASE-IV INHIBITOR
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Tartaric acid salts of (3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl) butanoyl]hexahydro-3-(2,2,2-trifluoroethyl)-2H-1,4-diazepin-2-one are potent inhibitors of dipeptidyl peptidase-IV and are useful for the prevention and/or treatment of non-insulin depe
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Page/Page column 10-11
(2008/06/13)
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