Synthetic method of degarelix

作者: Sun Meilu , Wang Xiaotao , Xu Feng , Zhou Jinyu , Gu Haitao

DOI:

关键词: Combinatorial chemistryTetrapeptideYield (chemistry)DegarelixChemistrySynthesis PeriodDrug synthesis

摘要: The invention relates to a synthetic method of degarelix, and belongs the field drug synthesis. A hexapeptide fragment R-D-Nal-D-Cpa-D-Pal-Ser(R1)-Aph(hor)-Aph(Cbm)(R2)-R3 tetrapeptide R-Leu-Lys(ipr)(R2)-Pro-D-Ala-R3 are condensed into Ac-D-Nal-D-Cpa-D-Pal-Ser(R1)-Aph(hor)-Aph(Cbm)(R2)-Leu-Lys(ipr)(R2)-Pro-D-Ala-R3 in presence condensating agent, then product degarelix is obtained through deprotection ammonolysis; or ammonolysis carried out on obtain degarelix. greatly shortens synthesis period, avoids 3-time feeding amount traditional solid-phase method, reduces cost mild reaction condition, high yield suitable for industrial production, purity.

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