芳基
卤化物
钯
胺气处理
化学
催化作用
卤代芳基
偶联反应
组合化学
有机化学
烷基
作者
Lei Xu,Fu-Yue Liu,Qi Zhang,Wei-Jun Chang,Zhonglin Liu,Ying Lv,Haizhu Yu,Jun Xu,Jianjun Dai,Hua‐Jian Xu
标识
DOI:10.1038/s41929-020-00564-z
摘要
Suzuki–Miyaura coupling is a practical and attractive carbon−carbon bond formation reaction due to its high efficiency and wide functional group compatibility, but its industrial applications are limited because it is typically catalysed by expensive palladium-containing transition-metal complexes. Here we show a robust and chemoselective organocatalytic Suzuki−Miyaura-type coupling of aryl halides with arylboronic acids catalysed by amines. The utility and scope of this reaction were demonstrated by the synthesis of several commercially relevant small molecules and a selection of derivatives of pharmaceutical drugs. The coupling of aryl halides and arylboronic acids is generally performed by metal-catalysed Suzuki–Miyaura reactions while metal-free approaches remain elusive. Here an organocatalytic approach based on amine catalysts is introduced for the preparation of commercially relevant asymmetric biaryls.
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