PROCESS FOR THE SYNTHESIS OF HISTIDYL-PROLINAMIDE DERIVATIVES USING POLYMERIC SOLID PHASE SUPPORT

摘要

PURPOSE: A method for preparing histidyl-proline amide derivative is provided to effectively remove by-products and to obtain the derivative of high purity. CONSTITUTION: A method for preparing histidyl-proline amide derivative of chemical formula 1 comprises: a step of coupling a polymer solid support having an amine group with nitrogen-protected proline or carboxylic acid-activated compound to obtain a coupled product of chemical formula 10; a step of deprotecting the nitrogen protection group and coupling with nitrogen group-protected histidine or carboxylic acid to obtain a coupled product of chemical formula 12; a step of deprotecting protection group P5 and coupling with a compound of chemical formula 2 or carboxylic acid-activated compound to obtain a coupled product of chemical formula 13; and a step of deprotecting protection group P4.