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

C - Chemistry – Metallurgy – 07 – J

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C07J 71/00 (2006.01) A61K 31/58 (2006.01) C07J 51/00 (2006.01)

Patent

CA 2096020

The present invention is directed to 2.beta.,19-(methyleneamino)androst-4-ene- 3,17-dione 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-methox- yethoxy)methylamino] steroid using titanium tetrachloride followed by, if desired, selective reduction of the 17-ketone.

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