Synthesis of 1-haloestradiols
US4676932A · kind A · utility
2Cited by
2References
3Claims
0Family size
Assignee
Inventors
Key dates
| Filing date | Dec 28, 1984 |
| Grant date | Jun 30, 1987 |
| Priority date | — |
| Expiry date | Dec 28, 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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.