1048703-14-5Relevant articles and documents
Practical asymmetric synthesis of Sitagliptin phosphate monohydrate
Gao, Haoling,Yu, Jiangang,Ge, Chengsheng,Jiang, Qun
, (2018/06/29)
Optically pure sitagliptin phosphate monohydrate is efficiently and practically synthesized through a chiral hemiacetal as the key intermediate in 54% overall yield starting from (E)-4-(2,4,5-trifluorophenyl)but-2-enal and N-boc-protected hydroxylamine. The chiral hemiacetal fragment is constructed by a tandem aza-Michael/hemiacetal reaction catalyzed by an organocatalyst and the influence of acidity of Br?nsted acid on tandem aza-Michael/hemiacetal reaction is researched in detail.
INTERMEDIATES OF SITAGLIPTIN AND PREPARATION PROCESS THEREOF
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, (2013/11/05)
Disclosed are intermediates of Sitagliptin, a preparation process thereof, and a process for synthesizing Sitagliptin using these intermediates. Sitagliptin is synthesized by using chiral amino compounds as a raw material, without having to build a chiral center with a chiral asymmetric catalytic hydrogenation, and high-pressure hydrogenation is avoided.
INTERMEDIATES OF SITAGLIPTIN AND PREPARATION PROCESS THEREOF
-
, (2013/10/22)
Disclosed are intermediates of Sitagliptin, a preparation process thereof, and a process for synthesizing Sitagliptin using these intermediates. Sitagliptin is synthesized by using chiral amino compounds as a raw material, without having to build a chiral center with a chiral asymmetric catalytic hydrogenation, and high-pressure hydrogenation is avoided.