OXYTOCIN ANALOGS AND METHOD FOR PREPARATION THEREOF

摘要

Analogs of oxytocin of general formula I (I), where all amino acids are L-isomers and X is phenylalanine or phenylalanine substituted in the p-position by alkyl, ethoxy, amino, substituted amino, or nitro group, suitable for medical applications, and a method for their preparation consisting in the cyclization of linear octapeptides of general formula II (II), where X has the aforesaid meaning and Act is a group activating the carboxylic group of S-carboxyethylhomocysteine residue, e.g. an active ester. Two methods may be used for the preparation of ¢2-p-aminophenylalanine ! deamino-6-carba-oxytocin, either the reduction of ¢2-p-nitrophenylalanine! deamino-6-carba-oxytocin or deprotection of ¢2-p-benzyloxy-carbonylaminophenylalanine ! deamino-6-carba-oxytocin.