Process for preparing des-proline vasopressin antagonists

Details Process for preparing des-proline vasopressin antagonists Process for preparing des-proline vasopressin antagonists

C - Chemistry, Metallurgy

07

K

530/7.14

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

Patent

CA 1249397

PROCESS FOR PREPARING DES-PROLINE VASOPRESSIN ANTAGONISTS Abstract of the Disclosure The des-proline VSP-peptides of this invention are prepared by methods using an oxidative cyclization of a 1,6-disulfhydryl linear peptide and, optional removal of any protecting group which may be present. These peptides, which have structures characterized by being a six unit cyclic peptide ring with a mono or dipeptide tail with no proline unit, have vasopressin antagonist activity. An important species of the group is [1-(B- mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(0-ethyl- D-tyrosine)-4-valine-7-desproline-8-arginine]-vasopressin.

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