Iodinated estradiols, intermediate products and methods of production
US4855125A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Sep 25, 1987 |
| Grant date | Aug 8, 1989 |
| Priority date | — |
| Expiry date | Sep 25, 2007 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61K2123/00
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
A method of preparation of estradiol derivatives labeled by iodine, especially .sup.123 I, substitution at C-16 are synthesized according to the present invention. A triflate intermediate is prepared from which either 16-alpha-.sup.123 I-17-beta-estradiol or 16-beta-.sup.123 I-17-beta-estradiol are prepared by described methods. Both 16-alpha-.sup.123 I- and 16-beta-.sup.123 I-17-beta-estradiol made according to the methods described herein have a high relative specific acitvity. The methods are sufficiently rapid so that the relatively short half-life of .sup.123 I is readily accommodated without substantial radioactive decay of the label.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.