Highly efficient asymmetric synthesis of sitagliptin

Authors :: Hansen, Karl B.
Yi Hsiao
Feng Xu
Rivera, Nelo
Clausen, Andrew
Kubryk, Michele
Krska, Shane
Rosner, Thorsten
Balsells, Jaume
Simmons, Bryon
Ikemoto, Nori
Yongkui Sun
Spindler, Felix
Malan, Christophe
Grabowski, Edward J.J.
Armstrong, Joseph D., III
Source :: Journal of the American Chemical Society. July 1, 2009, Vol. 131 Issue 25, 8798-8804
Publication Year :: 2009
Abstract: A highly efficient synthesis of sitagliptin, a potent and selective DPP-4 inhibitor for the treatment of type 2 diabetes mellitus (T2DM), is developed. The green synthesis has reduced the total waste generated per kilogram of sitagliptin produced in comparison with the first-generation route and has eliminated aqueous waste streams.