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钯催化的酰胺与芳基氯的直接分子间 α-芳基化反应。

Palladium-catalyzed direct intermolecular α-arylation of amides with aryl chlorides.

机构信息

Department of Applied Chemistry, China Agricultural University, Beijing 100193, P. R. China.

出版信息

Org Lett. 2013 Aug 16;15(16):4190-3. doi: 10.1021/ol4019002. Epub 2013 Aug 5.

Abstract

An efficient catalytic system for the direct intermolecular α-arylation of acetamide derivatives with aryl chlorides is presented. Chemoselectivities up to 10:1 in the mono- and diarylation of acetamides were achieved by careful selection of bases, solvents, and stoichiometry. Bis-arylated amides were prepared in up to 95% yield.

摘要

本文报道了一种用于酰胺衍生物与芳基氯的直接分子间α-芳基化的高效催化体系。通过仔细选择碱、溶剂和化学计量比,可以实现酰胺的单芳基化和二芳基化的化学选择性达到 10:1。双芳基化酰胺的产率高达 95%。

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