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Synthesis of Carmegliptin
S. Abrecht, J.-M. Adam, U. Bromberger, R. Diodone, A. Fettes*, R. Fischer, V. Goeckel, S. Hildbrand, G. Moine, M. Weber
F. Hoffmann-La Roche Ltd., Basel, Switzerland
20 July 2011 (online)
Carmegliptin is a dipeptidyl dipeptidase-IV inhibitor under development for the treatment of type-2 diabetes. Over 1000 kg was synthesized by the route depicted featuring an efficient crystallization-induced dynamic resolution of rac-D and a large-scale Hofmann rearrangement of the amide F.