Process for the preparation of 17-haloethynyl steroids, and...

Details Process for the preparation of 17-haloethynyl steroids, and... Process for the preparation of 17-haloethynyl steroids, and...

C - Chemistry, Metallurgy

07

J

260/2

C07J 1/00 (2006.01) C07J 5/00 (2006.01) C07J 7/00 (2006.01) C07J 17/00 (2006.01) C07J 41/00 (2006.01) C07J 51/00 (2006.01) C07J 63/00 (2006.01)

Patent

CA 1254883

ABSTRACT OF THE DISCLOSURE 17-haloethynyl steroids of the partial formula: Image wherein R1 is hydrogen or methyl, R2 is alkyl of 1-4 carbon atoms, acyl of 1-7 carbon atoms, trimethylsilyl, 2-tetrahy- dropyranyl, or nitrate, X is bromine or iodine, and V is methylene, ethylene, vinylene, ethylidene, vinylidene or cyclopropylene, can be prepared by treating an ethynyl steroid of the partial formula: Image wherein R1, R2, and V are as defined above, in an inert sol- vent with a brominating agent or an iodinating agent in the presence of a silver salt. The 17-haloethynyl steroids, some of which are novel have pharmacological activities similar to the an-halogenated steroids which are useful as intermediates in the preparation of the steroids.

452650

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