PRODUCTION OF PEPTIDE DERIVATIVE AND ITS INTERMEDIATE

摘要

PROBLEM TO BE SOLVED: To obtain a peptide derivative exhibiting an antioxytocin action and useful for preventing premature miscarriage, etc., by removing a protecting group from a specific carboxyl group-containing group-bound peptide derivative, and forming a cyclic structure with an amide bond in the molecule. SOLUTION: This method for producing a peptide derivative comprises oxidizing a compound (salt) of formula I (R<3> is a protecting group for the amino group of Ile; Acm is acetamide methyl) with a peroxide, reacting the product with a compound of formula II (MBz1 is 4-methoxybenzyl) in the presence of a sulfide compound to form a disulfide bond and remove the protecting group R<3> , reacting the obtained compound of formula III with a compound of the formula: R<2> -D-Trp(-R<1> )-OR<4> (R<1> is a protecting group for indolyl group of the formula) (D-Trp, H; R<2> is a protecting group for theα-amino group of D-Trp, R<4> is a protecting group for the carboxyl group of D-Trp), removing the protecting group R<2> from the obtained compound of formula IV and forming a cyclic structure with an intermolecular amide bond to obtain the peptide derivative of formula V.