各种缩合剂酸胺缩合机理详解

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    酰胺键广泛存在于天然产物和药物分子中,构建它们的方法多种多样,如经典的酸胺缩合,卤代烃的插羰反应,烷基胺的氧化反应等等。在众多方法中,酸胺缩合是合成中使用最广泛的方法之一。方法多种多样,缩合试剂也多种多样如HATU,EDCI,T3P,PyBOP,HBTU,DPPA等等。酸胺缩合虽然操作简单,反应也比较简单,但是反应中往往有不同的副产物,如何分析副产物就需要了解缩合的机理了。不同的缩合试剂有不同的反应机理,了解反应机理对我们分析反应中的副产物很有帮助。此外,酸胺缩合中手性产物的消旋也是我们非常关心的问题,如吖内脂的生成是众多消旋形成的主要原因之一。本文总结了多种缩合试剂的反应机理,核心机理是脱水过程,详见下图。







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