Process for preparing iodovinyl-estradiol
AssigneeThe George Washington University
InventorsIwao Nakatsuka, William Eckelman, Waclaw J. Rzeszotarski
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Abstract
17.alpha.-[(E)-2-Iodovinyl]-estra-1,3,5(10)-triene-3,17.beta.-diol wherein the iodine atom is radioactive can be produced from (E)-[3-acyloxy-17.beta.-hydroxyestra-1,3,5(10)-triene-17.alpha.-yl]vinyl dihydroxyborane in an excellent yield by iodinating the same and hydrolyzing the resulting 3-acyloxy-17.alpha.-[(E)-2-iodovinyl]-estra-1,3,5(10)-triene-17.beta.-ol.
Claims10
A process for preparing 17.alpha.-[(E)-2-iodovinyl]-estra-1,3,5(10)-triene-3,17.beta.-diol of the formula:
- ##STR4## which comprises iodinating (E)-[3-acyloxy-17.beta.-hydroxyestra-1,3,5(10)-triene-17.alpha.-yl]vinyl dihydroxyborane of the formula:
- ##STR5## wherein R is lower alkyl group having 1 to 4 carbon atoms, and hydrolyzing the resultant 3-acyloxy-17.alpha.-[(E)-2-iodovinyl]-estra-1,3,5(10)-triene-17.beta.-ol of the formula:
- ##STR6## wherein R is as defined above.
A compound selected from the group consisting of 3-acyloxy-17.alpha.-[(E)-2-iodovinyl]-estra-1,3,5(10)-triene-17.beta.-ol, 3-lower alkanoyloxy-17.alpha.-[(E)-2-iodovinyl]-estra-1,3,5(10)-triene-17.beta.-ol , 3-acetoxy-17.alpha.-[(E)-2-iodovinyl]-estra-1,3,5(10)-triene-17.beta.-ol and the corresponding compounds wherein the iodine atom is radioactive.
Dependencies are inferred from the claim text.