Organic compounds -- part of the class 532-570 series – Organic compounds – Polycyclo ring system containing anthracene configured ring...
Patent
1992-11-30
1995-04-11
Killos, Paul J.
Organic compounds -- part of the class 532-570 series
Organic compounds
Polycyclo ring system containing anthracene configured ring...
A61K 3158, C07D31196
Patent
active
054059798
DESCRIPTION:
BRIEF SUMMARY
This invention relates to a new process for the production of 10.beta.-H-11.beta.-(subst. phenyl) steroids of formula Ia ##STR2## or of formula Ib ##STR3## in which
R.sup.4 stands for a hydrogen atom, a cyano group, a chlorine, fluorine, bromine, iodine atom, for a trialkylsilyl, trialkylstannyl group, for a straight-chain or branched, saturated or unsaturated C.sub.1 -C.sub.8 alkyl, optionally protected acyl or alkoxyalkyl radical, for an amino group ##STR4## in which R.sup.7 and R.sup.8, independent of one another, mean a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group or for a corresponding amine oxide ##STR5## or for the groupings --OR.sup.9 or --S(O).sub.i R.sup.9 with i=0, 1 or 2, in which R.sup.9 means a hydrogen atom, a methyl, ethyl, propyl, isopropyl, methoxyphenyl, allyl or a 2-dimethylaminoethyl group, or for a heteroaryl radical of formula I.alpha. ##STR6## in which A symbolizes a nitrogen, oxygen or sulfur atom, -B-D-E-symbolizes the element sequence --C--C--C--, --N--C--C-- or --C--N--C-- and R.sup.10 symbolizes a hydrogen atom, a cyano group, a chlorine, fluorine, bromine, iodine atom, a trialkylsilyl, trialkylstannyl group, a straight-chain or branched, saturated or unsaturated C.sub.1 -C.sub.8 alkyl, optionally protected acyl or alkoxyalkyl radical, an amino group ##STR7## in which R.sup.7 and R.sup.8, independent of one another, mean a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, or a corresponding amine oxide ##STR8## or the grouping --OR.sup.9 or --S(O).sub.i R.sup.9 with i=0, 1 or 2 in which R.sup.9 means a hydrogen atom, a methyl, ethyl, propyl, isopropyl, methoxyphenyl, allyl or a 2-dimethylaminoethyl group, or for a heteroaryl radical of formula I.beta. ##STR9## in which A means a nitrogen atom and -B-D-E- means the element sequence --C--C--C--, --N--C--C--, --C--N--C-- --or C--C--N-- and R.sup.10 has the already indicated meaning, or for a phenyl radical of formula I.gamma. ##STR10## in which R.sup.10 has the already indicated meaning,
Y means a protected keto group or a protected hydroxy group and a hydrogen atom as well,
R.sup.1 means a hydrogen atom or a methyl group.
BACKGROUND OF THE INVENTION
In German patent application P 39 21 059.6, 11.beta.-aryl-4-estrenes of general formula I ##STR11## are described for the first time, in which
X stands for an oxygen atom, the hydroxy imino grouping >N OH or two hydrogen atoms,
R.sup.1 stands for a hydrogen atom or a methyl group,
R.sup.2 stands for a hydroxy group, a C.sub.1 -C.sub.10 alkoxy or C.sub.1 -C.sub.10 acyloxy group,
R.sup.3 stands for a hydrogen atom, the grouping --(CH.sub.2).sub.n CH.sub.2 Z, in which n is 0, 1, 2, 3, 4 or 5, Z means a hydrogen atom, the cyano group or the radical --OR.sup.5 with R.dbd..sup.5 H, C.sub.1 -C.sub.10 alkyl or C.sub.1 -C.sub.10 acyl, the grouping --(CH.sub.2).sub.m --C.tbd.C--Y, in which m means 0, 1 or 2 and Y means a hydrogen, fluorine, chlorine, bromine or iodine atom, a C.sub.1 -C.sub.10 hydroxyalkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.10 acyloxyalkyl radical, the grouping --CH.dbd.CH--(CH.sub.2).sub.k CH.sub.2 R.sup.6, in which k means 0, 1 or 2 and R.sup.6 means a hydrogen atom, a hydroxy group, a C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 acyloxy radical, or else R.sup.2 and R.sup.3 together stand for a radical of formula ##STR12##
R.sup.4 stands for a hydrogen atom, for a straight-chain or branched, saturated or unsaturated C.sub.1 -C.sub.8 alkyl, acyl or alkoxyalkyl radical, for an amino group ##STR13## in which R.sup.7 and R.sup.8, independent of one another, mean a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, or for a corresponding amine oxide ##STR14## or for the grouping --OR.sup.9, in which R.sup.9 means a hydrogen atom, a methyl, ethyl, propyl, methoxyphenyl, allyl or a 2-dimethylaminoethyl group, or for a heteroaryl radical of formula I.alpha. ##STR15## in which A symbolizes a nitrogen, oxygen or sulfur atom, -B-D-E-symbolizes the element sequence --C--C--C--, --N--C--C-- or --C--N--C-- and R.sup.10 symbolizes a hydrogen atom, a cyano, trialkylsilyl, tr
REFERENCES:
patent: 4357278 (1982-11-01), Quinkert et al.
Cleve Arwed
Neef Gunter
Ottow Eckhard
Wiechert Rudolf
Killos Paul J.
Schering Aktiengesellschaft
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