PRODUCTION OF PEPTIDE THIOL ESTER

摘要

PROBLEM TO BE SOLVED: To provide a production process for peptide thiol esters by using 9-fluorenylmethoxycarbonlated (Fmoc) amino acid. SOLUTION: In the thiol esterification process for peptide synthesis, an Fmoc- bonded terminal amino group in an amino acid that is immobilized through a thiol ester bond to a resin is removed with a specific Fmoc-removing reagent, another Fmoc-bonded amino acid is added to the exposed amino group, then the Fmoc group is eliminated. The addition of Fmoc-bonded amino acids to the immobilized polypeptide is repeated to prepare Fmoc-bonded peptide thiol ester resin. Then, the Fmoc group is removed and the polypeptide is removed from the immobilization resin, or the polypeptide is taken out of the immobilization resin followed by the deprotection of Fmoc group thereby, amino acids can be condensed into an arbitrary sequence.