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. 2020 Nov 16;12(5):704–712. doi: 10.1021/acsmedchemlett.0c00588

Scheme 1. Synthesis of Indole-2-carboxamides (Series I).

Scheme 1

Reagents and conditions: (i) R2-amine, EDC·HCl, HOBt, DIPEA, CH2Cl2 or DMF, rt, 3–12 h, 10–76%; (ii) BBr3, CH2Cl2, 0 °C to rt, 12 h, 81%; (iii) benzyl bromide, K2CO3, DMF, rt, 2 h, 21%.