School of Biotechnology and Health Sciences, Wuyi University, Jiangmen 529020, China.
J Org Chem. 2022 Sep 16;87(18):12214-12224. doi: 10.1021/acs.joc.2c01356. Epub 2022 Sep 2.
Practical copper-promoted -alkylation and bromination of arylamines/indazoles with alkyl bromides are described; the -alkylation-C-4-bromination and -dialkylation-C-4-bromination of arylamines, and -alkylation-C-3-bromination of indazoles, with alkyl bromides have been analyzed. The full use of alkyl bromides as alkylating and brominating building blocks without atom wastage, indicating excellent atom and step economy, has been highlighted. Eco-friendly oxygen and water are the reaction oxidant and byproduct, respectively.
本文描述了实用的铜促进的芳基胺/吲唑与烷基溴化物的-烷基化和溴化反应；分析了芳基胺的-烷基化-C-4-溴化和-二烷基化-C-4-溴化，以及吲唑的-烷基化-C-3-溴化与烷基溴化物的反应。充分利用烷基溴化物作为烷基化和溴化的构建块，没有原子浪费，表明具有出色的原子经济性和步骤经济性。环保的氧气和水分别是反应的氧化剂和副产物。
