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Cover Feature: Highly Enantioselective Synthesis of Sitagliptin (Asian J. Org. Chem. 2/2020)
Author(s) -
Khopade Kishor V.,
Sen Anirban,
Birajdar Rajkumar S.,
Paulbudhe Uday P.,
Kavale Dattatry S.,
Shinde Prashant S.,
Mhaske Santosh B.,
Chikkali Samir H.
Publication year - 2020
Publication title -
asian journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.846
H-Index - 44
eISSN - 2193-5815
pISSN - 2193-5807
DOI - 10.1002/ajoc.202000034
Subject(s) - enantioselective synthesis , sitagliptin , chemistry , sitagliptin phosphate , rhodium , catalysis , combinatorial chemistry , enamine , stereochemistry , organic chemistry , diabetes mellitus , type 2 diabetes mellitus , endocrinology , medicine
Diabetes is on the rise across the Globe and millions of people are being affected. Sitagliptin has emerged as a potent inhibitor for the treatment of type II diabetes, which can regulate blood sugar level, and new strategies to prepare this molecule are being discovered. Herein we report a highly enantioselective synthesis of sitagliptin. Using specifically identified chiral FerroLANE ligands in the presence of a rhodium catalyst the asymmetric hydrogenation of an enamine to yield sitagliptin with excellent enantioselectivity (98% ee ). The final product has been isolated as a phosphate salt with >99% ee . More information can be found in the Full Paper by Samir Chikkali et al. on page 189 in Issue 2, 2020 (DOI: 10.1002/ajoc.201900709).
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