Abstract

An efficient highly site-selective synthesis of 2,4,7-triarylpyrrolo[2,3-<i>d</i>]pyrimidines from 4-chloro-2-methylthiopyrrolo[2,3-<i>d</i>]pyrimidine has been developed. The proposed synthetic pathway is based on three sequential arylation reactions: Suzuki coupling at position 4 of pyrrolo[2,3-<i>d</i>]pyrimidine, copper(I)-catalyzed N(7)-arylation and nickel(0)-catalyzed desulfitative reaction of 2-methylthio group with aryl Grignard reagents.

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