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Synthesis of 4,7-Difunctionalized Indoles via Imino Exchange and Sulfinyl Migration

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journal contribution
posted on 23.01.2020, 13:33 by Xiaohua Li, Lei Li, Weiyi Wang, Qiuqin He, Renhua Fan
A process that rapidly assembles 4,7-difunctionalized indoles from 2-alkynycyclohexadienimines, sulfinamides, and nucleophiles (amines or alcohols) was developed. The process involves imino exchange, cascade cyclization/1,4-nucleophilic addition/aromatization, and 1,3-migration of the sulfinyl group. The 7-sulfinyl group is easy to convert into the sulfonyl or the thioether group through a simple oxidation and reduction reaction.