Process for preparing v.sub.1-vasopressin antagonists

Details Process for preparing v.sub.1-vasopressin antagonists Process for preparing v.sub.1-vasopressin antagonists

C - Chemistry, Metallurgy

07

K

530/7.14

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

Patent

CA 1249399

PROCESS FOR PREPARING V1-VASOPRESSIN ANTAGONISTS Abstract of the Disclosure Vasopressin derivatives having V1 and oxytocin antagonist activity whose structures are characterized by a Mpa unit at position 1 and a des-Pro unit at position 7 are prepared by peptide synthetic methods also using an oxidative cyclization of a dimercaptan. Representative species thusly prepared are [1-deaminopenicillamine-2- (0-methyl)-tyrosine-7-desproline-8-arginine-9-desglycine]- vasopressin or [1-.beta.-mercaptopropionic acid-2-D-(0-ethyl)- tyrosine-3-isoleucine-4-threonine-7-desproline-8-arginine-9- desglycine]vasopressin.

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