764667-65-4Relevant articles and documents
Two methods for the preparation of sitagliptin phosphate: Via chemical resolution and asymmetric hydrogenation
Ye, Fei,Zhang, Zhifeng,Zhao, Wenxia,Ding, Jianhai,Wang, Yali,Dang, Xueyan
, p. 4805 - 4809 (2021/02/03)
Two effective processes have been developed for the preparation of sitagliptin phosphate. The approach of chemical resolution obtained R-sitagliptin in five steps from commercially available starting materials using the inexpensive NaBH4 to reduce the enamine and then using (-)-di-p-toluoyl-l-tartaric acid to resolve racemates in 11% yield overall. The route successfully avoids the use of expensive noble metal as catalysts compared with traditional synthesis methods, resulting in greatly reduced costs and simplified synthetic routes. Other alternative asymmetric hydrogenation of β-ketomide routes for the synthesis of sitagliptin were found, two of the intermediates were synthesized for the first time. This journal is
Sitagliptin impurity as well as removal method and application thereof
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Paragraph 0046-0050, (2021/07/17)
The invention provides a sitagliptin impurity as well as a removal method and an application of the sitagliptin impurity, and particularly discloses an impurity in the production of a sitagliptin intermediate 4-oxo-4-[3-(trifluoromethyl)-5, 6-dihydro-[1, 2, 4] triazolo [4, 3-a] pyrazine-7-(8H)-yl]-1-(2, 4, 5-trifluorophenyl) butyl-2-ketone, and through the discovery of the impurity, the quality standard of sitagliptin or sitagliptin phosphate hydrate can be remarkably improved.
Method for preparing Sitagliptin intermediate
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, (2019/07/16)
The invention belongs to the field of organic synthesis and particularly relates to a method for preparing a Sitagliptin intermediate. The intermediate has a structure represented by a formula A shownin the description, wherein R1 and R2 are the same, or are differently hydrogen or C1-C5 alkyl, more preferably, R1 is tert-butyl, and R2 is hydrogen.