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US 2009/0156843 A1Published application
Process for aromatizing 19-norandrost-4-en-3-ones to estra-1,3,5(10)-trienes
OwnerMichael SANDER, Jorg Gries +1inventors
InventorsMichael SANDER, Jorg Gries, Armin Schutz
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Abstract
The present invention relates to a process for aromatizing 19-norandrost-4-en-3-ones (formula (II)) to astra-1,3,5(10)-trienes (formula (I))
Claims11
Process for CuBr2-mediated aromatization of 19-norandrost-4-en-3-ones of the general formula (II) to estra-1,3,5(10)-trienes of the general formula I
- where, in formula (II) and formula (I), each R is independently any chemically stable radical, characterized in that the aromatization is effected in the presence of at least one electron-rich, unsaturated organic additive of the general formula (Z)
- where
- R1, R2, R3, R4 are each independently hydrogen, a C1-C6-alkyl, C2-C6-alkenyl, C1-C6-alkoxy or C2-C6-alkenoxy radical or a C6-aryl ring or C6-aryloxy ring, with the proviso that at least one radical of R1, R2, R3, R4 is not hydrogen,
- or
- R1 and R2, together with the carbon atoms of the double bond, form a C6-aromatic optionally mono- or polysubstituted identically or differently by hydroxyl, a C1-C6-alkoxy radical and/or C1-C6-alkyl radical, a C3-C7-cycloalkene, a monocyclic heteroaromatic or an unsaturated heterocycle optionally additionally substituted by R3 and R4, where R3 and R4 are each independently a C1-C6-alkyl, C2-C6-alkenyl, C1-C6-alkoxy or C2-C6-alkenoxy radical, or a C6-aryl ring or C6-aryloxy ring,
- and enantiomers and diastereomers thereof.
3 more elements
Dependencies are inferred from the claim text.