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US 5,710,247 AGranted
Process and intermediates for the synthesis of LHRH antagonists
AssigneeAbbott Laboratories
InventorsKenneth W. Funk, Edwin O. Lundell, Robert B. Miller, Jane L. Chang, Vimal Kishore, James J. Napier, Michael A. Staeger
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Abstract
A method is provided for preparing decapeptide and undecapeptide derivatives of LHRH by solution phase peptide chemistry as well as intermediate peptides useful in the same method.
Claims18
A process for preparing an LHRH antagonist having the structure Q-D2Nal.sup.1 -D4ClPHe.sup.2 -D3Pal.sup.3 -Ser.sup.4 -NMeTyr.sup.5 -DLys(Nic).sup.6 -Leu.sup.7 -Lys(iPr).sup.8 -Pro.sup.9 DAla.sup.10 NH.sub.2 wherein Q is selected from the group consisting of N-acetyl and THF-Gly, comprising the steps of:
- (a) fully deprotecting a first protected oligopeptide compound having the formula
- P.sup.1 Ser(P.sup.2)-NMeTyr(P.sup.3)-D-Lys(Nic)-Leu-Lys(iPr)-pro-D-AlaNH.sub.2(IV)
- wherein P.sup.1 is an amino protecting group, and P.sup.2 and P.sup.3 are independently selected --OH protecting groups;
- and
- (b) coupling the unprotecting compound from step (a) with a second oligopeptide compound having the formula
- Q-D-2Nal-D-4ClPhe-D-3Pal-OH (III)
- to produce said LHRH antagonist.
4 more elements
Dependencies are inferred from the claim text.