Oxytocin analogs and method for preparation thereof

Details Oxytocin analogs and method for preparation thereof Oxytocin analogs and method for preparation thereof

C - Chemistry, Metallurgy

07

K

530/7.16

C07K 7/16 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1179328

ABSTRACT OF THE DISCLOSURE: Analogs of oxytocin of general formula I Image (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 Image (II), where X has the aforesaid meaning and Act is a group acti- vating 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.

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