Enantioselective synthesis of a GPR40 agonist AMG 837 via catalytic asymmetric conjugate addition of terminal alkyne to α,β-unsaturated thioamide

Ryo Yazaki, Naoya Kumagai, Masakatsu Shibasaki

研究成果: Article査読

44 被引用数 (Scopus)

抄録

A concise enantioselective synthetic route to a potent GPR40 agonist AMG 837 is described. The crucial catalytic asymmetric conjugate addition of terminal alkyne was promoted by a soft Lewis acid/hard Brønsted base cooperative catalyst, allowing efficient construction of the requisite stereogenic center. The thioamide functional group is key to both activation in asymmetric alkynylation and facile transformation into carboxylic acid.(Figure Presented)

本文言語English
ページ(範囲)952-955
ページ数4
ジャーナルOrganic Letters
13
5
DOI
出版ステータスPublished - 2011 3月 4
外部発表はい

ASJC Scopus subject areas

  • 生化学
  • 物理化学および理論化学
  • 有機化学

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