Ramachandran Kuppan, Anbarasan Pazhamalai
Department of Chemistry, Indian Institute of Technology Madras, Chennai 600036, India.
Org Lett. 2022 Sep 23;24(37):6745-6749. doi: 10.1021/acs.orglett.2c02527. Epub 2022 Sep 11.
An efficient rhodium-catalyzed synthesis of C2-alkylated NH-free indoles has been achieved from substituted indoles and cyclopropanols. The reaction allows the synthesis of various C2-alkylated products in good to excellent yield. Important features of the method include the use of a ,-dialkylcarbamoyl group as a traceless directing group, C-H/C-C bond functionalization, good functional group tolerance, broad scope, synthesis of pyrrolo[1,2-]indole, and identification of potential intermediates.
已实现了一种高效的铑催化从取代吲哚和环丙醇合成无C2-烷基化NH吲哚的方法。该反应能够以良好至优异的产率合成各种C2-烷基化产物。该方法的重要特征包括使用α,β-二烷基甲酰基作为无痕导向基团、C-H/C-C键官能化、良好的官能团耐受性、广泛的适用范围、吡咯并[1,2-a]吲哚的合成以及潜在中间体的鉴定。
