METHOD FOR SYNTHESIZING PEPTIDES

摘要

The present invention relates to a novel method for synthesizing peptides in solution, the method comprising: a) treating a peptide or amino acid derivative, which has an .alpha.-amine function blocked with a urethane grou p of the formula R1-SO2-CH2CH2-O-CO-, wherein R1 is aryl, with an excess of an aliphatic secondary amine in an organic solvent to provide the release of th e free .alpha.-amine function of said amino acid or peptide derivative and the formation of a tertiary amine adduct between said secondary amine and the liberated vinyl compound of the formula R1-SO2-CH2=CH2; b) removing the solvent and the excess of said secondary amine; c) contacting thus formed mixture of the N.alpha.-deprotected amino acid or peptide derivative and sai d tertiary amine adduct with subsequent peptide or amino acid derivative N.alpha.-protected with the above indicated or another urethane group under conditions providing the formation of a peptide bond between the free .alpha .- amine function of the N.alpha.-deprotected amino acid or peptide derivative and an .alpha.-carboxylic function of the subsequent N.alpha.-protected peptide or amino acid derivative; d) separating the newly formed peptide fro m the reaction mixture; e) repeating procedures as set forth above until the desired polypeptide is obtained.