Diverse O‐arylated pyrrolo[2,3‐d]pyrimidine and pyrrolo[2,3‐b]pyridine were obtained using relatively low amounts of Cu catalyst with ligand‐free conditions under microwave heating. The O‐arylation reaction could be applied to less oxidative heteroaryl‐chlorides. The microwave‐assisted Cu‐catalyzed O‐aryaltion would be useful for preparing potent bioactive compounds for drug discovery while reducing waste, time, and saving energy.
Facile introduction of diverse substituents to 2-or 4-chloro-7H-pyrrolo [2,3-d] pyrimidines was examined with microwave-assisted nucleophilic substitution and Cu-catalyzed N-arylation. Microwave-assisted Cu-catalyzed N-arylation of pyrrolo[2,3-d]pyrimidines with various nucleophiles proceeded very well with diverse heteroaryl halides. Sequential microwave-assisted substitution provided good to excellent yields of 2,7-or 4,7-disubstituted pyrrolo[2,3-d]pyrimidines, with short reaction times and energy savings compared with conventional thermal heating. The diverse pyrrolo[2,3-d]pyrimidine derivatives are useful for screening drug candidates for various diseases.
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