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Synfacts 2011(6): 0586-0586
DOI: 10.1055/s-0030-1259892
DOI: 10.1055/s-0030-1259892
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag
Stuttgart ˙ New York
Synthesis of AMG 837
R. Yazaki, N. Kumagai*, M. Shibasaki*
Institute of Microbial Chemistry, Tokyo and The University of Tokyo, Japan
Further Information
Publication History
Publication Date:
19 May 2011 (online)

Significance
Agonists of the G-protein-coupled receptor GPR40 amplify insulin secretion from the pancreas. AMG 837 (J) is a GPR40 agonist that is a potential treatment for type-2 diabetes. Shibasaki and co-workers report a short, enantioselective synthesis of AMG 837 that features an asymmetric conjugate addition of ethynyltrimethylsilane (B) to the α,β-unsaturated thioamide A promoted by a soft Lewis acid/hard Brønsted base cooperative catalyst.