2.beta.,19-methyleneamino bridged steroids as aromatase inhibito

Details 2.beta.,19-methyleneamino bridged steroids as aromatase inhibito 2.beta.,19-methyleneamino bridged steroids as aromatase inhibito

1990-11-30

1992-06-30

Bond, Robert T.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Cyclopentanohydrophenanthrene ring system doai

540 49, 540 91, 552505, C07J 7100, C07J 5100, A61K 3158

Patent

active

051264889

ABSTRACT:
The present invention is directed to 2.beta.,19-(methyleneamino)androst-4-ene-3,17-dione which has the formula ##STR1## and the corresponding 17.beta.-ol which are useful as aromatase inhibitors. The compounds are prepared by the cyclization of an appropriate 19-[N-protected-[(2-methoxyethoxy)methylamino] steroid using titanium tetrachloride followed by, if desired, selective reduction of the 17-ketone.

REFERENCES:
patent: 4322416 (1982-03-01), Metcalf et al.
Johnson, et al., Endocrinology 115(2), 1984 pp. 776 to 785.
Burkhart, Steroids 45(3,4), 1985 pp. 357-374.
Lan-Hargest et al., Tetrahedron Letters, 28, 6117 (1987).
Grenway et al., Biochemistry International, 20, 591 (1990).
Eggleston et al., Chemical Abstracts, 109, 139666j (1988).

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