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    • 98. 发明专利
    • BR6570119D0
    • 1973-08-02
    • BR17011965
    • 1965-06-02
    • BRITISH DRUG HOUSES LTD
    • THE BRITISH DRUG HOUSES LTD
    • A61K31/568A61K31/569A61K31/57A61K31/573A61K31/575A61K31/58C07J1/00C07J5/00C07J13/00C07J71/00C07J75/00
    • The invention comprises 6-hydroxymethyl-3oxo-D 4,6-steroids and their acylates; and their preparation by treatment of 3-enol ethers of 6hydroxymethyl - 3 - oxo - D 4 - steroids or their acylates (the etherifying group being an alkyl, chloralkyl, hydroxyalkyl, cycloalkyl or aralkyl radical) with dehydrogenating reagents; or by reaction of 3-enol alkyl ethers of 6-hydroxymethyl-3-oxo-D 4-steroids or their acylates with acids of at most 6 carbon atoms with an equivalent amount of a halogen in an inert solvent and in the presence of at least an equivalent amount of a strong proton acceptor; and the preparation of the 6-acyloxy compounds wherein the acyl group contains at most 10 carbon atoms by treatment of the 6-hydroxymethyl compounds with acylating reagents. The steroids which may be used as starting materials are those described in Specification 929,984 (including derivatives of testololactone) or the 6-acylates thereof, prepared by acylation. Quinones are suitable dehydrogenating reagents. Examples are given and the preparation of some starting materials by the method disclosed in Specification 929,984 is also described, as is hydrolysis of some products containing a 6-acyloxymethyl group to the 6-hydroxymethyl compounds.ALSO:A pharmaceutical preparation comprises a 6-hydroxy- or acyloxy-methyl-3-oxo-4, 6-dienic steroid in admixture with one or more solid or liquid pharmaceutically acceptable inert carriers and, if desired, an oestrogen. These preparations are stated variously to have anabolic, androgenic, gonadotrophin inhibiting, claudagenic, progestational, anti-inflammatory and anti-endotoxic properties and, when they contain an oestrogen, to be of value as oral contraceptives. They may take the form of pills or tablets, an example of the latter containing 17 a -acetoxy-6-hydroxymethylpregna-4, 6-diene-3, 20-dione and ethynyloestradiol being given.