Synthesis of 2-hydroxyestradiol derivatives
US6448419B1 · kind B1 · utility
8Cited by
1References
9Claims
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Key dates
| Filing date | Aug 7, 2001 |
| Grant date | Sep 10, 2002 |
| Priority date | — |
| Expiry date | Aug 7, 2021 |
Classification
- Technology area (CPC Y)Emerging Cross-Sectional Technologies
- CPC primaryY02P20/55
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Disclosed is a method of preparing 2-hydroxy-3,17&bgr;-estradiol derivatives wherein 3,17&bgr;-estradiol is reacted with an organolithium reagent and reacted with either a boron reagent or a silicon reagent to form either a 2-boronyl or a 2-silyl modified estradiol analog represented by the corresponding structural formulae: R1 and R2 are each independently a hydroxyl protecting group. R3, R4 and R5 are selected from the group consisting of halogens, alkyl, aryl, hydroxy, substituted or unsubstituted alkyl, and substituted or unsubstituted aryl.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.