A new synthetic route to triaryl pyrrolo[2,3‐d]pyrimidines from common 4,6‐dichloropyrimidine has been developed. The triarylated compounds are synthesized by three cross‐coupling reactions using three different catalysts. The introduction of a C‐6 aryl group was achieved in a two‐step process under Sonogashira conditions [Pd(dba)2/CuI] followed by intramolecular cyclization, and application of Suzuki–Miyaura conditions [Pd(PPh3)4; PdCl2(PPh3)2] led to C‐4 and C‐5 diarylation. This sequence allows a flexible synthetic approach to highly arylated pyrrolopyrimidines containing different aryl groups.
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