| 摘要 |
The invention comprises a compound having the formula <FORM:1055534/C2/1> and the corresponding D 4,6 compounds wherein X is hydrogen, methyl, fluoro, chloro, trifluoromethyl, difluoromethyl or fluoromethyl; R is <FORM:1055534/C2/2> with the proviso that when X is fluoro, chloro, trifluoromethyl, difluoromethyl or fluoromethyl, R must be <FORM:1055534/C2/3> R1 is hydrogen or the acyl radical of a hydrocarbon monocarboxylic acid containing from 1-12 carbon atoms, and R2 is the acyl radical of a hydrocarbon carboxylic acid containing 1-12 carbon atoms and a process for the preparation thereof (1) by reacting compounds of Formula (I) <FORM:1055534/C2/4> and the corresponding 6-dehydro analogues thereof wherein X, R and R2 are as defined above, with a metal hydride reducing agent to obtain the compounds of Formula (II), <FORM:1055534/C2/5> and the corresponding 6-dehydro analogues thereof; and (2) then if desired acylating the compounds of Formula II, and the corresponding 6-dehydro analogues thereof, with an acylating agent to obtain the compounds of Formula (III), <FORM:1055534/C2/6> and the corresponding 6-dehydro analogues thereof, wherein X, R1 and R2 are as defined above and R3 is the acyl radical of a hydrocarbon carboxylic acid containing 1-12 carbon atoms. As reducing agent there may be employed lithium aluminium tri-t-butoxide.ALSO:Pharmaceutical compositions effective as antifertility, estrus regulating, progestational, pregnancy maintaing and anti-inflammatory agents and containing a compound of the formula: <FORM:1055534/A5-A6/1> or the corresponding D 4,6 compound (wherein X is hydrogen, methyl, fluoro, chloro, trifluoromethyl, difluoromethyl, or fluoromethyl, R is <FORM:1055534/A5-A6/2> with the proviso that when X is fluoro chloro, trifluoromethyl, difluoromethyl or fluoromethyl, R must be <FORM:1055534/A5-A6/3> , R1 is hydrogen or the acyl radical of a hydrocarbon monocarboxylic acid containing 1-12 carbon atoms and R2 is the acyl radical of a hydrocarbon carboxylic acid containing from 1-12 carbon atoms) are administered orally as pills, tablets, capsules, syrups, or elixirs, in liquid forms for injection, or topically as ointments, lotions, creams with coacting antibiotics and germicides.
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