| 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:
€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ (P 1 )AA 1 -AA 2 -AA 3 -AA 4 (P 4 )-AA 5 -AA 6 (P 6 )-AA 7 -AA 8 (P 8 )-AA 9 -AA 10 -NH 2 €ƒ€ƒ€ƒ€ƒ€ƒ(II)
or a salt or solvate thereof,
to a treatment with a cleaving agent in an organic solvent,
wherein
P 1 is an amino protecting groups; preferably acetyl;
P 4 is hydrogen or a hydroxyl protecting group, preferably a hydroxyl protecting group;
P 6 is hydrogen or an amino protecting groups; preferably an amino protecting groups; and
P 8 is an amino protecting group. |
