Abstract
Reaction of estradiol-17β with triethylamine-sulfur trioxide in pyridine gives exclusively monosulfation at the C17-hydroxyl group with the preparation of 17β-sulfooxyestra-1,3,5(10)-trien-3-ol triethylammonium salt (V). The structural assignment suggested by spectroscopic measurements was confirmed by synthetic studies. ▪ A synthesis of 3-sulfooxyestra-1,3,5(10)-trien-17β-ol triethylammonium salt (II) has been accomplished based on the preparation of 17β-formyloxyestra-1,3,5(10)-trien-3-ol (XIII). Fusion of the 3-sulfate triethylammonium salt II gives rise to the 17-sulfate triethylamine salt V. The preparation of estradiol-17β disulfate has also been achieved.
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