Liu Haiyan, Li Zheng
College of Chemistry and Chemical Engineering, Northwest Normal University, Lanzhou, Gansu 730070, P. R. China.
Org Lett. 2021 Nov 5;23(21):8407-8412. doi: 10.1021/acs.orglett.1c03133. Epub 2021 Oct 11.
A method for the synthesis of benzo[4,5]imidazo[2,1-]isoquinolines through Sonogashira cross-coupling/nucleophilic addition tandem reactions using calcium carbide as a solid alkyne source, 2-(2-bromophenyl)benzimidazoles as starting materials, and copper as a catalyst is described. The target products can also be synthesized through one-pot three-component reactions of -phenylenediamines, -bromobenzaldehydes, and calcium carbide. Both reaction routes can also be scaled up to gram scale.
描述了一种通过使用碳化钙作为固体炔源、2-(2-溴苯基)苯并咪唑作为起始原料以及铜作为催化剂，经由Sonogashira交叉偶联/亲核加成串联反应合成苯并[4,5]咪唑并[2,1-]异喹啉的方法。目标产物也可以通过对苯二胺、邻溴苯甲醛和碳化钙的一锅三组分反应来合成。两条反应路线都可以放大到克级规模。
