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钯催化的未反应的 C(sp)-H 键与唑 C(sp)-H 键的交叉偶联反应,使用溴化物作为无痕迹导向基团。

Palladium-catalyzed cross-coupling of unreactive C(sp)-H bonds with azole C(sp)-H bonds by using bromide as a traceless directing group.

机构信息

The Research Center of Chiral Drugs, Innovation Research Institute of Traditional Chinese Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, P. R. China.

出版信息

Chem Commun (Camb). 2022 Jun 8;58(46):6661-6664. doi: 10.1039/d2cc01944b.

Abstract

A palladium-catalyzed intermolecular cross-coupling of unreactive C(sp)-H bonds and azole C(sp)-H bonds with bromide as a traceless directing group is described. The judicious selection of the bulky and electron-rich phosphine ligand is the key for the success of this cascade process. The protocol features a broad substrate scope, excellent regioselectivity, and good functional group tolerance.

摘要

描述了一种钯催化的不活泼 C(sp)-H 键和唑 C(sp)-H 键与溴化物的分子间交叉偶联反应,溴化物作为无痕迹导向基团。选择大位阻和富电子膦配体是此级联反应成功的关键。该方案具有广泛的底物范围、优异的区域选择性和良好的官能团耐受性。

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