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Synthesis of Sitagliptin
K. B. Hansen*, Y. Hsiao*, F. Xu*, N. Rivera, A. Clausen, M. Kubryk, S. Krska, T. Rosner, B. Simmons, J. Balsells, N. Ikemoto, Y. Sun, F. Spindler, C. Malan, E. J. J. Grabowski, J. D. Armstrong, III
Merck Research Laboratory, Rahway, USA and Solvias AG, Basel, Switzerland
20 November 2009 (online)
Sitagliptin is the active antihyperglycemic ingredient in JANUVIA and JANUMET both of which were recently approved by the FDA for the treatment of type 2 diabetes. It is a selective inhibitor of dipeptidyl peptidase IV (DPP-4). The route depicted has been implemented on a manufacturing scale and is a major improvement on the first-generation route (K. B. Hansen et al. Org. Process Res. Dev. 2005, 9, 634).