Process for the preparation of 4-amino-.DELTA..sup.4 -3-ketoster

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai

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514178, 514179, 514181, 552515, 552522, A61K 3156, C07J 4100

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active

059655500

ABSTRACT:
The invention discloses 3-ketosteroids of the following formula used to inhibit steroid C.sub.17-20 lyase: ##STR1## wherein R is OH, C.sub.1 -C.sub.6 alkanoyl, C.sub.1 -C.sub.6 alkanoyloxy, C.sub.1 -C.sub.4 alkanol, COCH.sub.2 OH, CO.sub.2 H, CONR.sub.7 R.sub.8, cyclopropyloxy, cyclopropylamino, acetylthioalkane, 2,2-dimethyldioxolan4-yl, 1,2-dihydroxyethyl and C.sub.1-4 alkylthiol;

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patent: 5143909 (1992-09-01), Weintraub et al.
patent: 5218110 (1993-06-01), Weintraub
J. Chem Soc, Perkin Trans. 1; 1988 No. 12 pp. 3239-3242 "Synthesis of new nitro and amino sterols; potential inhibitors of 4-methyl sterol oxidase." Letchworth GB.
Ind. Chem. Library, Advances in Organobromine Chemistry, vol. 3, 1991 pp. 119-125 "Synthesis of novel aromatase inhibitors from bromosteroidal intermediates." Longo, et al.aromatase inhibitors from bromosteroidal intermediates. Longo, et al.
Curran et al., A novel route to a 4-amino steroid, Tetrahedron Lett., 36(27),4761-4 Abstract only, 1995.
Weintraub et al., A Novel Route to a 4-Amino Steroid: MDL 19687, Tetrahedron lett. vol. 36, No. 27, pp. 4761-4764, 1995.

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