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Highly Enantioselective Synthesis of Sitagliptin
Journal article   Peer reviewed

Highly Enantioselective Synthesis of Sitagliptin

Kishor Khopade, Anirban Sen, Rajkumar S. Birajdar, Uday P. Paulbudhe, Dattatry S. Kavale, Prashant S. Shinde, Santosh B. Mhaske and Samir H. Chikkali
Asian journal of organic chemistry, Vol.9(2), pp.189-191
01/02/2020
DOI: https://doi.org/10.1002/ajoc.201900709

Abstract

Chemistry Chemistry, Organic Physical Sciences Science & Technology
A highly enantioselective synthesis of sitagliptin, a potent DPP-4 inhibitor, is reported. Explicitly identified chiral FerroLANE ligands in the presence of rhodium catalyze the asymmetric hydrogenation of an enamine to yield sitagliptin with excellent enantioselectivity (98% ee). The process was scaled up to 5 g and the final product was isolated as a phosphate salt with >99% ee.

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