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银催化杂芳烃与叔环烷醇的C2选择性直接烷基化反应。

Silver-catalyzed C2-selective direct alkylation of heteroarenes with tertiary cycloalkanols.

作者信息

Lu Shi-Chao, Li Hong-Shuang, Xu Shu, Duan Gui-Yun

机构信息

State Key Laboratory of Bioactive Substance and Function of Natural Medicines, and Beijing Key Laboratory of Active Substance Discovery and Drugability Evaluation, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, No. 1 Xiannongtan Street, Beijing 100050, P R China.

School of Pharmaceutical Sciences, Taishan Medical University, 619 Changcheng Road, Taian 271016, P R China.

出版信息

Org Biomol Chem. 2017 Jan 4;15(2):324-327. doi: 10.1039/c6ob02330d.

Abstract

A silver-catalyzed regioselective C2-alkylation of heteroarenes with tertiary cycloalkanols under radical conditions was developed. This tandem process, which includes selective C-H activation, C(sp)-C(sp) bond cleavage, and C(sp)-C(sp) bond formation, affords a novel and environmentally friendly approach for the production of carbonyl-containing alkyl-substituted heteroarenes with moderate to good yields.

摘要

开发了一种在自由基条件下银催化杂芳烃与叔环烷醇的区域选择性C2-烷基化反应。这个串联过程包括选择性C-H活化、C(sp)-C(sp)键断裂和C(sp)-C(sp)键形成,为生产含羰基的烷基取代杂芳烃提供了一种新颖且环境友好的方法,产率适中至良好。

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