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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… Click to show full abstract
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.
Journal Title: Organic letters
Year Published: 2020
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