Peptide Synthesis Of L-Prolyl-L-Leucyl-Glycinamide Using Mixed-Carbonic Anhydride Method

Tripeptide L-Prolyl-L-Leucyl-Glycinamide(PLG), as a Melanocyte Stimulating Hormone-inhibiting Hormone(MIH),has been reported to have some useful physiological and pharmacological functions. Composed to other methods ,this paper used Mixed-Carbonic Anhydride Method to synthesis PLG, and discussed reaction factors. It mainly included:(1) In the paper, PLG peptide was synthesized with L-Pro, L-Leu and Glycinamide using Mixed-Carbonic Anhydride Method. In this method, the Amido of L-Pro and L-Leu were firstly protected by Carbobenzoxy and then the Carbobenzoxy was removed by Pd/C.(2) Through the orthogonal experiments, the optimum experimental conditions for the reaction of Amido protected by Carbobenzoxy were attained.(3) Different effects on the synthesis of PLG peptide using Mixed-Carbonic Anhydride Method were discussed in this paper. The experimental results indicated that PLG peptide with high O.P. could be synthesized at the following conditions: Isobutyl chlorormate as mixed anhydride at -10℃.