Synthesis of a mixture of sulfated estrogens using a sulfur trioxide complex
OwnerThomas W. Leonardinventor
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Abstract
A process of producing a stable composition comprising a mixture of sulfated estrogens. The mixture of sulfated estrogens may comprise sulfated alkali metal salts of Δ8,9-dehydroestrone, estrone, and derivatives thereof or other estrogens. The process comprises the steps of sulfating such mixture of alkali metal salts of Δ8,9-dehydroestrone, estrone, and derivatives thereof with a sulfur trioxide complex and adding tris(hydroxymethyl)aminomethane.
Claims19
A process for the production of a stable composition comprising a mixture of sulfated estrogens, the process comprising the steps of:
- a) reacting a sulfur trioxide complex with a mixture of alkali metal salts of estrogens to provide a mixture of sulfated alkali metal salts of estrogens;
- b) adding a stabilizing amount of tris(hydroxymethyl)aminomethane;
- and
- c) recovering the stable composition comprising the mixture of sulfated estrogens and tris(hydroxymethyl)aminomethane.
A process for the production of a stable composition comprising a mixture of sulfated estrogens, the process comprising the steps of:
- a) reacting a mixture of estrogens with sodium hydride in an apolar, aprotic solvent to provide a mixture of alkali metal salts of the estrogens;
- b) reacting sulfur trioxide-trimethylamine with the mixture of alkali metal salts of estrogens in an apolar, aprotic solvent to provide a mixture of sulfated alkali metal salts of estrogens;
- c) adding a stabilizing amount of tris(hydroxymethyl)aminomethane;
- and
- d) recovering the stable composition comprising the mixture of sulfated estrogens and tris(hydroxymethyl)aminomethane.
Dependencies are inferred from the claim text.