PROCESS FOR THE PREPARATION OF 7 alpha -(METHOXYCARBONYL)-3-OXO-17alpha-PREGN-4,9(11)-DIEN-21,17-CARBOLACTONE, A USEFUL INTERMEDIATE FOR THE SYNTHESIS OF MOLECULES WITH PHARMACOLOGICAL ACTIVITY
AssigneeIndustriale Chimica S.R.L.
InventorsRoberto Lenna, Riccardo Di Brisco, Francesco Barbieri
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Abstract
An improved process for the preparation of intermediate (V) through the elimination of a molecule of water from intermediate (IV) is described. Intermediate (V) is a key molecule for the synthesis of eplerenone, a synthetic steroid with pharmacological activity used in the treatment of chronic pathological conditions, including hypertension.
Claims3
A process for the production of 7α-(methoxycarbonyl)-3-oxo-17α-pregn-4-9 (11)-dien-21,17-carbolactone (V) comprising the elimination of a molecule of water from 11α-hydroxy-7α-(methoxycarbonyl)-3-oxo-17α-pregn-4-en-21,17-carbolactone (IV) by reaction with the mixture (VI) (Et)2NCF2CHFCF3/(Et)2NFC═CFCF3, wherein the amounts of the two components of said mixture (VI) are variable in ratios such that, in a gas chromatographic analysis, the area of the minority component is not less than 75% of the area of the majority component.
Dependencies are inferred from the claim text.