Direct Imine Acylation: Rapid Access to Diverse Heterocyclic Scaffolds
Direct Imine Acylation: Rapid Access to Diverse Heterocyclic Scaffolds
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DOI：
10.1021/ol303073b
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发表时间：
2013-01-18
期刊：
影响因子：
5.2
通讯作者：
Taylor, Richard J. K.
中科院分区：
文献类型：
--
作者：
Unsworth, William P.;Kitsiou, Christiana;Taylor, Richard J. K.
描述了一种简单而有效的方法，通过使用各种官能化苯甲酸直接酰化亚胺来制备一系列不同的杂环。该方法采用了一种新的方法来产生N-酰亚胺离子，然后由氧、氮、硫和碳基亲核试剂在分子内原位捕获。本文还报道了用ReactIR进行的初步机理研究。
A simple and efficient procedure to prepare a range of diverse heterocycles by the direct acylation of imines using a variety of functionalized benzoic acids is described. The methodology features a novel method for N-acyliminium ion generation followed by in situ intramolecular trapping by oxygen-, nitrogen-, sulfur- and carbon-based nucleophiles. Preliminary mechanistic studies, using ReactIR, are also reported.