Patent · US Active

Ganirelix precursor and method for preparing ganirelix acetate by using the same

US10577394B2 · kind B2 · utility

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20Claims
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Key dates

Filing dateJun 12, 2015
Grant dateMar 3, 2020
Priority date
Expiry dateJan 14, 2036

Classification

  • Technology area (CPC Y)Emerging Cross-Sectional Technologies
  • CPC primaryY02P20/55
  • WIPO fieldBiotechnology
  • WIPO sectorChemistry

Abstract

Disclosed is a method for preparing ganirelix acetate. The method includes the following steps: respectively replacing Fmoc-HArg(Et)2-OH and Fmoc-D-HArg(Et)2-OH by employing Fmoc-Lys(Boc)-OH and Fmoc-D-Lys(Boc)-OH or Fmoc-Lys(Alloc)-OH and Fmoc-D-Lys(Alloc)-OH; synthesizing a ganirelix precursor I or ganirelix precursor II-peptide resin in advance; and then respectively performing modifications and treatments on side chain amino groups of Lys and D-Lys in the precursor I or the precursor II-peptide resin to obtain ganirelix acetate. The ganirelix acetate synthesized therefrom is high in purity, has few impurities and a relatively low cost, and is suitable for large-scale production.

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