METHOD FOR PRODUCTION OF PEPTIDE THIOESTER COMPOUND

摘要

Disclosed is a method for production of a peptide thioester compound, which comprises the following steps (A) to (C): (A) forming a peptide by a solid phase synthesis method using a resin modified with a linker represented by the formula (1) as a solid phase; (B) cleaving the bond between the solid phase and the peptide with at least one acid selected from dilute hydrochloric acid, dilute sulfuric acid and acetic acid to produce a peptide having a carboxyl group at the C-terminus; and (C) reacting the resulting peptide with a thiol compound in a solvent in the presence of a condensing agent at -100 to 0º to produce the peptide thioester compound. (1) wherein R¹ represents a C_1-4 alkyl group; R² represents a hydrogen atom or a C_1-4 alkoxy group; and n represents an integer of 1 to 4.