Halogen labeled compounds including estradiol derivatives, their

Details Halogen labeled compounds including estradiol derivatives, their Halogen labeled compounds including estradiol derivatives, their

1984-10-22

1987-04-21

Roberts, Elbert L.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

424 11, A61K 4300, C07J 100

Patent

active

046595171

ABSTRACT:
A method of preparation of halogen labeled organic compounds is described. In particular, estradiol derivatives labeled by halogen substitution at C-16 are synthesized according to the present invention. A triflate intermediate is prepared from which either 16-alpha-halo-substituted-17-beta-estradiols or 16-beta-halo-substituted-17-beta-estradiols can be rapidly formed as desired. In particular, the preparation of 16-alpha-.sup.123 I-17-beta-estradiol and 16-beta-.sup.123 I-17-beta-estradiol are shown and are synthesized from a 17-beta-estradiol-16-beta-triflate. Both 16-alpha-.sup.123 I- and 16-beta-.sup.123 I-17-beta-estradiol made according to the present invention are shown to have a high specific activity. The method of synthesis is sufficiently rapid so that the relatively short half-life of .sup.123 I is readily accommodated. The high stereospecificity of each step of the reaction sequence in preparing the labeled estradiols provides for highly efficient syntheses and little waste of radio-label.

REFERENCES:
patent: 4465676 (1984-08-01), Hochberg
McElvany et al., "J. Nucl. Med 23 (1982), pp. 420-424.
Chemical Abstracts, vol. 98, No. 25, Jun. 20, 1983, p. 586, No. 215878b, Therain et al.
Journal of Organic Chemistry, vol. 49, No. 25, Dec. 14, 1984, pp. 4900-4905, Kiesewelter et al.
Journal Biological Chemistry, vol. 245, No. 13, (1979), pp. 5900-5905, Arunachalam et al.

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