Amino Acids and Peptides. VII. Synthesis of Methionine-Enkephalin using Transfer Hydrogenation

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Catalytic transfer hydrogenation was examined with several proton donors for removal of the Z group from Z-Met-OBu^t. cis-Decalin as well as cyclohexene was a good proton donor for transfer hydrogenation. Met-enkephalin was synthesized by the same route as Leu-enkephalin in combination with Z group and tert-butyl ester group for protection, with removal of the Z group by transfer hydrogenation. The biological activity of the synthetic peptides as determined by measuring the inhibition of electrically evoked contraction of the guinea pig ileum was in good agreement with the results reported with the natural materials, indicating that this method may be useful for the synthesis of Metcontaining biologically active peptides.