[摘要]:The modified Ugi reaction has been developed to synthesize tripeptides containing alpha,alpha-diphenylglycine (Dph) together with bulky amino acids. By the use of diphenylmethanimine, N-benzyloxycarbonyl (Z) amino acids and isocyanides derived from amino acids, very crowded tripeptides such as Z-Aib-Dph-AibOMe, Z-Ac(6)c-Dph-Aib-OMe, Z-Dph-Dph-Dph-OMe, etc. have been synthesized.