1380243-35-5Relevant articles and documents
Efficient synthesis of sitagliptin phosphate, a novel DPP-IV inhibitor, via a chiral aziridine intermediate
Pan, Xianhua,Li, Xiaojun,Lu, Qingling,Yu, Wansheng,Li, Weijin,Zhang, Qunhui,Deng, Fei,Liu, Feng
, p. 6807 - 6809 (2013)
Sitagliptin phosphate, a novel DPP-IV inhibitor of T2DM, has been synthesized via 12 linear steps, in an overall yield of 26%. The key step is the coupling reaction of 2,4,5-trifluorophenylmagnesium bromide with a chiral aziridine derivative, which was prepared from l-homo-serine by simple steps.
INTERMEDIATES OF SITAGLIPTIN AND PREPARATION PROCESS THEREOF
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, (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.