Weak Chelation-Assisted C4-Selective Alkylation of Indoles with Cyclopropanols via Sequential C-H/C-C Bond Activation.

Tripti Paul, Shubhajit Basak, Tharmalingam Punniyamurthy

Organic letters 2022 Aug 19

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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.

Citation

Tripti Paul, Shubhajit Basak, Tharmalingam Punniyamurthy. Weak Chelation-Assisted C4-Selective Alkylation of Indoles with Cyclopropanols via Sequential C-H/C-C Bond Activation. Organic letters. 2022 Aug 19;24(32):6000-6005