METHOD FOR PRODUCTION OF PEPTIDE THIOESTER COMPOUND

摘要

The present invention provides a process for producing a peptide thioester compound, characterized by comprising: (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 a bond between the solid phase and the peptide with at least one acid selected from dilute hydrochloric acid, dilute sulfuric acid, formic acid, and acetic acid to produce a peptide having a carboxyl group at the C-terminus; and (C) reacting a thiol compound with the peptide at -100 to 0°C in the presence of a condensing agent in a solvent: (1) wherein R 1 represents C 1-4 alkyl group, R 2 represents hydrogen atom or C 1-4 alkoxy group, and n represents an integer of 1 to 4.