Synfacts 2009(5): 0478-0478  
DOI: 10.1055/s-0028-1088170
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of a Dipeptidyl Peptidase 4 Inhibitor

Contributor(s): Philip Kocienski
Z. Fei*, Q. Wu, F. Zhang, Y. Cao, C. Liu, W.-C. Shieh*, S. Xue, J. McKenna, K. Prasad*, M. Prashad, D. Baeschlin, K. Namoto
Suzhou Novartis Pharma Technology Co., Changshu, P. R. of China; Novartis Pharmaceuticals Corporation, East Hanover, USA; Novartis Institutes for Biomedical Research, Basel, Switzerland
Further Information

Publication History

Publication Date:
22 April 2009 (online)

Significance

The target molecule is in development for the treatment of type 2 diabetes because it inhibits dipeptidyl peptidase 4 (DPP-4) leading to a reduction in elevated blood glucose levels. The key step in the synthesis is an asymmetric ­nucleophilic addition of Grignard reagent E to the N-tert-butanesulfinimine D.