Ganirelix precursor and method for preparing ganirelix acetate by using the same
US10577394B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Jun 12, 2015 |
| Grant date | Mar 3, 2020 |
| Priority date | — |
| Expiry date | Jan 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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.