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US 6,933,395 B1Granted
Processing for producing of drospirenone (6β, 7β, 15β, 16β-dimethylene-3-oxo-17α-pregn-4-en-21, 17-carbolactone, drsp) as well as 7α-(3-hydoxy-1-proply)-6β, 7β; 15β, 16β-dimethylene-5β-androstane-3β, 5,17β-triol(zk 92836) and 6β, 7β; 15β, 16β-dimethylene-5β-hydroxy
AssigneeSchering Corporation
InventorsJörg-Thorsten Mohr, Klaus Nickisch
Life of this patent
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Abstract
Process for the production of drospirenone (6β,7β; 15β,16β-dimethylene-3-oxo-17α-pregn-4-ene-21,17-carbolactone, DRSP) (1) and 7α-(3-hydroxy-1-propyl)-6β,7β; 15β,16β-dimethylene-5β-androstane-3β,5,17β-triol (ZK 92836) and 6β,7β; 15β,16β-dimethylene-5β-hydroxy-3-oxo-17α-androstane-21,17-carbolactone (ZK 90965) as intermediate products of the process.
Claims6
A composition comprising 6β,7β;
- 15β,16β-dimethylene-3-oxo-17α-pregn-4-ene-21,17-carbolactone, a pharmaceutically acceptable carrier, and less than 0.2% weight of said compound of contaminants
A composition comprising 6β,7β;
- 15β,16β-dimethylene-3-oxo-17α-pregn-4-ene-21,17-carbolactone, a pharmaceutically acceptable carrier, and less than 0.2% by weight of said compound of the contaminants
- wherein X is an anion acid which is effective to open said 6β,7β-methylene group.
A composition comprising
- 6β,7β;
- 15β,16β-dimethylene-3-oxo-17α-pregn-4-ene-21,17-carbolactone made by a process comprising dehydrating a compound of Formula III,
- which was made by oxidizing in the presence of a ruthenium salt a compound of formula
- which was made by catalytically hydrogenating a compound of formula I
- (b) a pharmaceutically acceptable carrier, and
- (c) less than 0.2% by weight of said compound (a) of the by products of said preparation process which are
- wherein X is anion of an acid which is effective to open said 6β,7β-methylene group.
4 more elements
6β,7β;
- 15β,16β-dimethylene-5β-hydroxy-3-oxo-17α-androstane-21,17-carbolactone
- in isolated form.
6β,7β;
- 15β,16β-dimethylene-5β-hydroxy-3-oxo-17α-androstane-21,17-carbolactone
- in isolated form.
Dependencies are inferred from the claim text.