The Research Center of Chiral Drugs, Innovation Research Institute of Traditional Chinese Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, P. R. China.
Chem Commun (Camb). 2022 Jun 8;58(46):6661-6664. doi: 10.1039/d2cc01944b.
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.
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。