Synthesis of 1-haloestradiols
US4584137A · kind A · utility
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25Claims
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Key dates
| Filing date | Apr 9, 1984 |
| Grant date | Apr 22, 1986 |
| Priority date | — |
| Expiry date | Apr 9, 2004 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07J41/0011
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Estrogens characterized by an aromatic ring of the formula ##STR1## are halogenated by electrophilic substitution of a halo atom at the 1-position of the aromatic ring after protection of the sensitive 3-hydroxyl substituent and amination at the 4-position. Preferred starting materials include estrones or derivatives thereof. The estrones are preferably reduced after masking and amination to form the corresponding estradiols, which are then halogenated, deaminated and deprotected to provide the novel 1-haloestradiols.
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