通过亲核芳香取代反应实现酯、内酯、酰胺和内酰胺的α-杂芳基化。
Alpha-heteroarylation of esters, lactones, amides, and lactams by nucleophilic aromatic substitution.
作者信息
Shen Hong C, Ding Fa-Xiang, Colletti Steven L
机构信息
Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Company, Inc., P.O. Box 2000, Rahway, New Jersey 07065-0900, USA.
出版信息
Org Lett. 2006 Mar 30;8(7):1447-50. doi: 10.1021/ol060246u.
PMID:16562913
Abstract
[reaction: see text] A mild and efficient alpha-heteroarylation of simple esters and amides was developed via nucleophilic aromatic substitution. The choice of NaHMDS in toluene gave the best results. A tandem alpha-heteroarylation and hydroxylation protocol using air as the oxidant afforded tertiary alcohols in good yields.
摘要
[反应：见正文] 通过亲核芳香取代反应，开发了一种温和且高效的简单酯和酰胺的α-杂芳基化反应。在甲苯中选择NaHMDS可得到最佳结果。使用空气作为氧化剂的串联α-杂芳基化和羟基化反应方案以良好的产率得到叔醇。
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