| 摘要 |
Disclosed is a liquid-phase process for preparing Degarelix having the formula Ac-AA1-AA2-AA3-AA4-AA5-AA6-AA7-AA8-AA9-AA10-NH2 or a pharmaceutically acceptable salt or solvate thereof, wherein AA1 is D-2Nal, AA2 is D-4Cpa, AA3 is D-3Pal, AA4 is Ser, AA5 is 4Aph(L-Hor), AA6 is D-Aph(Cbm), AA7 is Leu, AA8 is Lys(iPr), AA9 is Pro and AA10 is D-Ala, comprising the step of subjecting a Degarelix precursor according to formula II or a salt or solvate thereof to a treatment with a cleaving agent, wherein formula II is as disclosed in the specification. Also disclosed are polypeptide intermediates useful in the solution-phase manufacturing process and to the purification of Degarelix itself. |
