Process for iodinating or brominating the alpha-methylenic carbon of a secondary amide
申请人:MERCK & CO. INC.
公开号:EP0473225A2
公开(公告)日:1992-03-04
A novel, facile, and specific process for α-iodinating or α-brominating the α-methylenic carbon of a straight chain, branched chain, or cyclic secondary amide, such as a lactam or an azasteroid, comprises reacting the amide with trialkylsilyl-X (R₃Si-X), where X is Br, I, or Cl, and R is methyl, ethyl, or n-propyl, in the presence of I₂ or Br₂. The α-iodo- or α-bromo-amide is useful for making the α,β-unsaturated amide through dehydrohalogenation.
一种用于对直链、支链或环状仲酰胺的 α-亚甲基碳进行 α-碘化或 α-溴化的新颖、简便和特异的工艺、例如内酰胺或氮杂环丁烷,包括在 I₂ 或 Br₂ 存在下,使酰胺与三烷基硅烷-X (R₃Si-X)反应,其中 X 是 Br、I 或 Cl,R 是甲基、乙基或正丙基。α-碘或 α-溴酰胺可用于通过脱氢卤化制得 α,β-不饱和酰胺。