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Details for Patent: 5,288,717

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Details for Patent: 5,288,717

Title: Alkali metal 8,9-dehydroestrone sulfate esters
Abstract:This invention presents alkali metal salts of 8,9-dehydroestrone, its sulfate ester, and stable compositions thereof, as well as processes for their production. The sulfate ester salts are useful in estrogen replacement therapy.
Inventor(s): Raveendranath; Panolil C. (Plattsburgh, NY), Wichtowski; John A. (St. Albans, VT)
Assignee: American Home Products Corporation (Madison, NJ)
Filing Date:Dec 03, 1992
Application Number:07/984,741
Claims:1. An alkali metal salt of 8,9-dehydroestrone.

2. A salt of claim 1 which is the sodium salt of 8,9-dehydroestrone.

3. A salt of claim 1 which is the potassium salt of 8,9-dehydroestrone

4. A salt of claim 1 which is the lithium salt of 8,9-dehydroestrone.

5. A process for the production of a stable composition containing an alkali metal salt of 8,9-dehydroestrone-3-sulfate which comprises reacting trimethylamine-sulfurtrioxide with an alkali metal salt of 8,9-dehydroestrone in a polar, aprotic solvent in the presence of a stabilizing amount of tris(hydroxymethyl)aminomethane.

6. A process for the production of a stable composition containing an alkali metal salt of 8,9-dehydroestrone-3-sulfate which comprises reacting trimethylamine-sulfurtrioxide with an alkali metal salt of 8,9-dehydroestrone in a polar, aprotic solvent, adding a stabilizing amount of tris(hydroxymethyl)aminomethane to the reaction mixture, and recovering said stable mixture of alkali metal salt of 8,9-dehydroestrone and tris(hydroxymethyl)aminomethane.
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