One-pot synthesis of 4-aminated pyrrolo[2,3-d]pyrimidines from alkynylpyrimidines under metal-catalyst-free conditions

A novel, general, and efficient one-pot sequential reaction toward a variety of 4-aminated-6-arylpyrrolo[2,3-d]pyrimidines from 5-alkynylpyrimidines has been developed. Microwave-assisted metal-free intramolecular cyclization and amination provided moderate to excellent yields of 4-aminated pyrrolo[2,3-d]pyrimidines in short reaction times. This method avoids the use of metal-catalyst and expensive additives and was shown to tolerate amines and anilines.