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Synfacts 2009(12): 1303-1303  
DOI: 10.1055/s-0029-1218332
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of Sitagliptin

Contributor(s): Philip Kocienski
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
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Publication History

Publication Date:
20 November 2009 (online)

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Significance

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).