Abstract

Rapid microwave-assisted solution-phase peptide synthesis protocol has been developed. The reaction temperature of 50°C, 40W and short coupling time of 28min gave racemization-free synthesis of peptides in 50–80% yield. The method is applicable with equal ease in coupling both side-chain protected and unprotected amino acids indicating reactive-functional group tolerance and high atom-economy. In the case of dipeptides, DIC/HONB-mediated coupling rendered the best results. In the case of tri- and tetrapeptides, HATU/HOAt/DIEA emerged as the best coupling combination.

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