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Details for Patent: 4,650,610

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Details for Patent: 4,650,610

Title: Androstane carbothioic acids
Abstract:Androstane carbothioic acids of the formula: ##STR1## wherein R.sup.1 represents a hydrogen atom, a hydroxy group in the .alpha.-configuration, a methyl group which may be in either the .alpha.- or .beta.-configuration, or a methylene group; R.sup.2 represents a hydroxy or protected hydroxy group in either the .alpha.- or .beta.-configuration or an oxo group; R.sup.3 represents a hydrogen, bromine, chlorine or fluorine atom; or R.sup.2 and R.sup.3 together represent a carbon-carbon bond or an epoxy group in the .beta.-configuration; R.sup.4 represents a hydrogen or fluorine atom; and the symbol represents a single or double bond and the salts thereof are useful as intermediates in the preparation of anti-inflammatory androstane 17.beta.-carbothioate esters. The compounds of formula I are prepared by reaction of a reactive derivative of a 17.beta.-carboxylic acid corresponding to the compound of formula I with hydrogen sulphide or a sulphide or hydrosulphide salt.
Inventor(s): Phillipps; Gordon H. (Wembley, GB2), Bain; Brian M. (Chalfont St. Peter, GB2), Laing; Stuart B. (Harrow, GB2)
Assignee: Glaxo Group Limited (London, GB2)
Filing Date:Jul 10, 1985
Application Number:06/753,428
Claims:1. A compound of the formula ##STR10## wherein R.sup.1 represents a hydrogen atom, a hydroxy group in the .alpha.-configuration, a methyl group which may be in either the .alpha.- or .beta.-configuration, or a methylene group;

R.sup.2 represents a hydroxy or protected hydroxy group in either the .alpha.- or .beta.-configuration or an oxo group;

R.sup.3 represents a hydrogen, bromine, chlorine or fluorine atom; or R.sup.2 and R.sup.3 together represent a carbon-carbon bond or an epoxy group in the .beta.-configuration;

R.sup.4 represents a hydrogen or fluorine atom; and the symbol represents a single or double bond; and the salts thereof.

2. A compound according to claim 1 wherein R.sup.1 represents a hydrogen atom, a methyl group in either the .alpha.- or .beta.-configuration, or a methylene group.

3. A compound according to claim 1 wherein R.sup.1 represents a methyl group in the .alpha.- or .beta.-configuration or a methylene group, R.sup.2 represents a hydroxy group in the .beta.-configuration or an oxo group; R.sup.3 represents a fluorine atom; R.sup.4 represents a hydrogen atom or a fluorine atom and the symbol represents a carbon-carbon double bond and the salts thereof.

4. A compound according to claim 1 selected from the group consisting of:

9.alpha.-Fluoro-11.beta.,17.alpha.-dihydroxy-16.beta.-methyl-3-oxoandrosta- 1,4-diene-17.beta.-carbothioic acid and the salts thereof;

9.alpha.-Fluoro-17.alpha.-hydroxy-16.beta.-methyl-3,11-dioxoandrosta-1,4-di ene-17.beta.-carbothioic acid and the salts thereof;

9.alpha.-Fluoro-11.beta.-17.alpha.-dihydroxy-16.alpha.-methyl-3-oxoandrosta -1,4-diene-17.beta.-carbothioic acid and the salts thereof;

9.alpha.-Fluoro-17.alpha.-hydroxy-16.alpha.-methyl-3,11-dioxoandrosta-1,4-d iene-17.beta.-carbothioic acid and the salts thereof;

9.alpha.-Fluoro-11.beta.,17.alpha.-dihydroxy-16-methylene-3-oxoandrosta-1,4 -diene-17.beta.-carbothioic acid and the salts thereof; and

9.alpha.-Fluoro-17.alpha.-hydroxy-16-methylene-3,11-dioxoandrosta-1,4-diene -17.beta.-carbothioic acid and the salts thereof.

5. 6.alpha.,9.alpha.-Difluoro-11.beta.,17.alpha.- dihydroxy-16.alpha.-methyl-3-oxoandrosta-1,4-diene-17.beta.-carbothioic acid and the salts thereof.

6. 6.alpha.,9.alpha.-Difluor o-17.alpha.-hydroxy-16.alpha.-methyl-3,11-dioxoandrosta-1,4-diene-17.beta.- carbothioic acid and the salts thereof.
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