Patent ID: 6747125
Filing Date: 2004-06-08
Classification: A61K,C07C,C07D,C07K,Y10S

Abstract:
A peptide intermediate for making a GnRH antagonist peptide which intermediate has the formula:Ac-AA1-(4Cl)D-Phe-AA3-Ser(X3)-aminoPhe(Xa)-D-aminoPhe(Xa)-Leu-Lys(Ipr,X6)-Pro-D-Ala-NH-resin support, wherein AA1 is &bgr;-D-NAL, (A)D-Phe or (B)D-Trp; A is H, 4Cl, 4F, 4NO2, 4CH3, 4OCH3, C&agr;Me/4Cl, 2,4 Cl2 or 4Br; B is H, 6NO2; 6NH2, 6OCH3, 6F, 6Cl, 6Br, 6CH3, 1Acetyl or 1Formyl; AA3 is D-PAL, &bgr;-D-NAL or (B)D-Trp, X3 is hydrogen or a protecting group for a hydroxyl group of Ser; Xa is a protecting group for a side chain primary amino group which protecting group is base-labile, hydrazine-labile or thio-labile; and X6 is benzyloxycarbonyl or 2-chlorobenzyloxycarbonyl.