4.6 Article

Synthesis of 2-acetal-1,3-enynes by Sonogashira reaction of bromovinyl acetals with alkynes: application to the formal synthesis of a glucagon antagonist

期刊

NEW JOURNAL OF CHEMISTRY
卷 46, 期 24, 页码 11492-11501

出版社

ROYAL SOC CHEMISTRY
DOI: 10.1039/d2nj01541b

关键词

-

资金

  1. Ministere de l'Enseignement Superieur
  2. Centre National de la Recherche Scientifique

向作者/读者索取更多资源

Functionalized 1,3-enynes bearing an acetal moiety at the 2-position were prepared through Sonogashira reaction. The reaction showed excellent substrate tolerance and could be easily scaled up. This method has important application in the synthesis of a key intermediate for glucagon antagonist.
The preparation of functionalized 1,3-enynes bearing an acetal moiety at the 2-position has been studied through Sonogashira reaction of bromovinyl acetals with various alkyl- and aryl-substituted terminal alkynes. The palladium-catalyzed coupling reaction tolerated a wide substrate scope and a range of 2-acetal-1,3-enynes were obtained in up to 87% yield under mild conditions that could be transposed to multi-gram scale. This protocol has been applied to the preparation of a key intermediate in the synthesis of a glucagon antagonist.

作者

我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。

评论

主要评分

4.6
评分不足

次要评分

新颖性
-
重要性
-
科学严谨性
-
评价这篇论文

推荐

暂无数据
暂无数据