Study on the Synthesis of N-methyldipeptide N-Ns-N (Me)-L-Ala-N (Me)-L-Ile-OtBu
A N-methylated peptide amide bond often exhibits higher resistance to proteolysis and thus results in improved oral activity and enhanced duration of action. However, few N-methyl amino acids are commercially available and their synthesis is tedious. The formation of hindered amide bond with high yield and minimal racemization is often troublesome. Herein the hindered N-methyl-dipeptide ( N-Ns-N( Me) -L-Ala-N( Me) -L-Ile-O'Bu) , a segment of the new cyclodepsipeptide Apratoxin A, which exhibits cytotoxycity against human tumor cell lines, was synthesized from L-Alanine and L-iso-Leucine through ten steps. The coupling reaction needs not any catalyst and proceeds effectively, so the workup procedure is quite simple.
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