1174122-54-3Relevant articles and documents
Intermediate of DPP-IV inhibitor, preparation method thereof and method of preparing DPP-IV inhibitor through intermediate
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Paragraph 0092; 0093; 0094; 0095, (2017/07/19)
The invention relates to an intermediate of a DPP-IV inhibitor (as shown in a formula I), a preparation method thereof and a method of preparing the DPP-IV inhibitor through the intermediate. The method of preparing the DPP-IV inhibitor specifically comprises the following steps of: performing a reaction on a cyclic chiral beta-amino aryl butyric acid derivative (as shown in a structural formula I) and a compound III; and then removing an amido protecting group to prepare the needed DPP-IV inhibitor. The method provided by the invention is simple and convenient to operate, low in cost and suitable for large-scale production. The formula is as shown in the description.
Preparation method of 3R-amino substituted butyrylamide derivative
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Paragraph 0083; 0087, (2016/10/09)
The invention relates to a preparation method of a 3R-amino substituted butyrylamide derivative. The preparation method of the 3R-amino substituted butyrylamide derivative comprises the following steps: carrying out hydrogenation reduction on enamine II for preparing 3R,3S-amino substituted butyrylamide racemate III; carrying out resolution, and filtering, so as to obtain 3R-amino substituted butyrylamide R(-) mandelate with high ee% value, alkalifying to obtain the 3R-amino substituted butyrylamide derivative; and oxidizing the obtained mother liquor, so as to obtain enamine II in a recycling manner, and repeating oxidation-reduction cycle for multiple times until products at specified yield are obtained. The preparation method of the 3R-amino substituted butyrylamide derivative has the advantages that a cyclic method is utilized for converting 3S-amino substituted butyrylamide racemate or 3R,3S-amino substituted butyrylamide mixture in any ratio into the 3R-amino substituted butyrylamide derivative with high ee% value, so that the mother liquor is effectively utilized; meanwhile, an expensive catalyst or asymmetric reductive amination with high demand condition does not need to be adopted, thereby being beneficial to reduction of cost and clean production.
Salts of Methyl (R)-7-[3-Amino-4-(2,4,5-Trifluoro-Phenyl)-Butyryl]-3-Trifluoromethyl-5,6,7,8-Tetrahydro-Imidazo[1,5-A]Pyrazine-1-Carboxylate
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Page/Page column 2-3, (2012/05/21)
The pharmaceutically acceptable salts of methyl (R)-7-[3-amino-4-(2,4,5-trifluoro-phenyl)-butyryl]-3-trifluoromethyl-5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine-1-carboxylate, their preparation methods and their use for preparing anti-diabetic medicaments a