| 摘要 |
The present invention relates to a liquid (or solution)-phase manufacturing process for preparing the decapeptide Degarelix, its protected precursor, and other useful intermediates. The invention further relates to polypeptides useful in the solution-phase manufacturing process and to the purification of Degarelix itself. Degarelix can be obtained by subjecting a Degarelix precursor according to formula (II): (P1)AA1-AA2-AA3-AA4(P4)-AA5-AA6(P6)-AA7-AA8(P8)-AA9-AA10-NH2 (II) or a salt or solvate thereof, to a treatment with a cleaving agent in an organic solvent, wherein P1 is an amino protecting groups; preferably acetyl; P4 is hydrogen or a hydroxy! protecting group, preferably a hydroxyl protecting group; P6 is hydrogen or an amino protecting groups; preferably an amino protecting groups; and P8 is an amino protecting group.
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