Syntheses of (R)-sitagliptin

In the last 10 years, since Merck’s discovery and development of (R)-sitagliptin phosphate as a treatment for type 2 diabetes, numerous efforts towards efficient synthesis of (R)-sitagliptin have been reported. In this review, several total syntheses of (R)-sitagliptin are described, highlighting the key stereoselective and stereospecific strategies employed.

Graphical abstractA review of the syntheses of (R)-sitagliptin, a dipeptidyl peptidase IV (DPP-4) inhibitor for the treatment of type 2 diabetes, is presented.Figure optionsDownload full-size imageDownload as PowerPoint slide