Department of Chemistry, Innovative Drug Research Center, Shanghai University , Shanghai 200444, China.
Org Lett. 2014 Oct 17;16(20):5294-7. doi: 10.1021/ol502447w. Epub 2014 Sep 24.
An unexpected rhodium-catalyzed regioselective C-H chlorination of 7-azaindoles was developed using 1,2-dichloroethane (DCE) as a chlorinating agent and 7-azaindole as the directing group. This protocol provides an efficient access to ortho-chlorinated azaindoles with operational simplicity, good functional group tolerance, and a wide substrate scope.
发展了一种铑催化的 7-氮杂吲哚的区域选择性 C-H 氯化反应，使用 1,2-二氯乙烷（DCE）作为氯化试剂，7-氮杂吲哚作为导向基团。该方法具有操作简单、官能团容忍性好、底物适用范围广等优点，为邻位氯化的氮杂吲哚提供了一种有效的合成途径。
