Department of Chemistry, Indian Institute of Technology Guwahati, Guwahati 781039, India.
Org Lett. 2022 Aug 19;24(32):6000-6005. doi: 10.1021/acs.orglett.2c02265. Epub 2022 Aug 10.
A Rh-catalyzed weak chelation-guided C4-alkylation of indoles has been accomplished using cyclopropanols as an alkylating agent via the cascade C-H and C-C bond activation. The substrate scope, functional group tolerance, and late-stage mutation of drug molecules are the important practical features.
实现了 Rh 催化的弱螯合导向吲哚 C4-烷基化反应,使用环丙醇作为烷基化试剂,通过级联 C-H 和 C-C 键活化。底物范围、官能团耐受性和药物分子的后期突变是重要的实际特征。