Patent ID: 7816489
Filing Date: 2010-10-19
Classification: A61K,C07C,C07K

Abstract:
1. A method for preparing a peptide or a pharmaceutically acceptable salt thereof, having oxytocin antagonist activity and consisting of a moiety A and a residue B having a C-terminal β-aminoalcohol which is bound to the moiety A by an amide bond, wherein (1) said residue B is: with Q being (CH (2) said moiety A is: with Mpa, Ile, Asn and Abu having the following meanings: (a) reacting an α-amino acid having a protected amino side chain and an acylated α-amino group with a reducing agent to change the acyl group to an alkyl group and to simultaneously change the α-carboxy group to CH 2 OH to provide a diamino alcohol having the formula: wherein P (b) reacting said product of step (a) with the pentapeptide: wherein P 4 , P 5 and P 6 are individually protecting groups to form the linear hexapeptide: c) selectively deprotecting and cyclizing the linear compound of step(b) to create the heptapeptide: