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    • 6. 发明专利
    • PROCESS FOR PRODUCTION OF NEW STEROID-SPIRO-LACTONS
    • HUT34763A
    • 1985-04-28
    • HU298883
    • 1983-08-26
    • GYOGYSZERKUTATO INTEZET
    • SZILAGYI GEZANESOLYOM SANDORTOLDY LAJOSSCHAEFER INGENAGYNE IVOCS JUDITNAGYNE BALOGH MARIA
    • C07J1/00C07J21/00C07J31/00
    • Novel steroidal-spiro-lactones of general formula (I) and their salts obtd. by opening the lactone ring, are prepd. by reacting a cpd. of general formula (IV) in the presence of a base with a malonic-acid-dialkyl-ester with 1-3 carbons. In the formulae R1 is hydrogen or methyl, R2 is alkyl with 1-3 carbons, R3 is hydrogen or 1-3C alkyl-thio gp. or 2-4C alkanoyl-thio gp. Z is a gp. of formula (II) or (III), X is H or 2-4C alkoxy-carbonyl with 2-4 carbons. M is metal. The dotted line between carbons 6 and 7 can mean an additional valency bond, with the proviso, that if the dotted line does stand for an additional bond, R3 can only be hydrogen. - If in the prod. of formula (I) resulting from the reaction X is an alkoxy-carbonyl gp. and Z is a gp. of formula (II), the cpd. of formula (I) is opt. heated in the presence of water. If in the resulting cpd. of formula (I) R3 is hydrogen, the dotted line between carbons 6 and 7 does not mean an additional bond, Z stands for a gp. of formula (II) with X meaning hydrogen, a further valency bond can opt. be produced in the 6(7) position of the stern structure using a benzo-quinone deriv. Alternatively an alkyl-mercaptan with 1-3 carbons or a thiol-carboxylic-acid with 2-4 carbons can be opt. additioned to the double bond in position 6(7), and/or salt can opt. be formed with the equiv. amt. of alkali from cpds. of formula (I) when Z means a gp. of formula (II) and X stands for hydrogen.