Process for the synthesis of gonadotropin releasing hormone antagonists
US6620824B2 · kind B2 · utility
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4References
28Claims
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Key dates
| Filing date | Apr 5, 2002 |
| Grant date | Sep 16, 2003 |
| Priority date | — |
| Expiry date | Apr 5, 2022 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D453/06
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The present invention relates to a process for preparing a compound of gonadotropin releasing hormone antagonists having a Formula I, in an efficient way, which involves preparation of key intermediates: 2-arylindole core; a chiral aziridine, in particular chiral nosyl aziridine; and an amine salt. The key process involves the coupling reaction of 2-arylindole and nosyl aziridine under boron trifluoride catalysis, which provides the final compound with unprecedented regioselectivity and enantioselectivity.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.