Drug – bio-affecting and body treating compositions – Radionuclide or intended radionuclide containing; adjuvant...
Patent
1987-09-25
1989-08-08
Schenkman, Leonard
Drug, bio-affecting and body treating compositions
Radionuclide or intended radionuclide containing; adjuvant...
2603975, 514182, A61K 4300, A61K 3156, C07J 100
Patent
active
048551252
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.
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Baranczuk Richard J.
Duncan William P.
Rotert Gary A.
Spicer Jay
Bio-Medical Research Laboratories
Lipovsky Joseph A.
Schenkman Leonard
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