Process for the preparation of methyl 6-(2,4-dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylate
US12157721B2 · kind B2 · utility
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28Claims
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Key dates
| Filing date | Mar 5, 2021 |
| Grant date | Dec 3, 2024 |
| Priority date | — |
| Expiry date | Jul 10, 2043 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07C59/255
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Herein is provided a novel process for the preparation of methyl 6-(2,4-dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylate by a Suzuki coupling of compound (3), wherein LG represents a leaving group, with an organoboron reagent: Compound (3) is obtained by activation of compound (4) with a leaving group LG, and compound (4) is obtained by alpha-arylation of methyl 5-oxo-6,7,8,9-tetrahydro-5H-benzo[7]annulene-2-carboxylate with 1-LG′-2,4-dichlorobenzene, wherein LG′ represents a leaving group:
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.