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

摘要

The present invention is directed to 2 beta ,19-(methyleneamino)androst-4-ene-3,17-dione which has the formula IMAGE 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.