C - Chemistry – Metallurgy – 07 – J
Patent
C - Chemistry, Metallurgy
07
J
167/193, 167/47,
C07J 1/00 (2006.01) A61K 31/565 (2006.01) A61K 49/00 (2006.01) C07J 15/00 (2006.01) C07J 51/00 (2006.01)
Patent
CA 1310631
ABSTRACT OF THE DISCLOSURE 17.alpha.-bromo-.alpha.and 17.alpha.-iodo-vinyl-estrane derivatives of general formula I Image (I), wherein X is a bromine or iodine atom in Z or E position, R1 is hydrogen, hydroxy or acyloxy with up to 3 C atoms, R2 is hydrogen, alkyl with up to 3 C atoms and alkanoyl and aroyl with up to 7 C atoms, R3 is hydrogen or methyl, R4 is a hydrogen atom in the .alpha. or .beta. position, R5 is hydrogen, methyl or methoxy and R6 is hydrogen or methyl, are pharmacologically effective with a profile of action like ethinylestradiol and in the form of their radioactively labeled compounds are also valuable diagnostic media. The z-isomers can be prepared by a new process by reaction of the corresponding 17.alpha.-ethinyl steroids with trialkyl(or phenyl)tin hydride with addition of a free radical former.
487352
Elger Walter
Grill Hans-Jorg
Hofmeister Helmut
Laurent Henry
Pollow Kunhard
Marks & Clerk
Schering Aktiengesellschaft
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