(17)-Alkynyl-(17)-hydroxy-(4,15)-oestradienones and derivs. - progestational agents inhibiting ovulation and implantation

摘要

Steroids of formula (I) are new: (R1 = H, trialkylsilyl or acyl. R2 = ethynyl, chloroethynyl or propynyl. X is oxo, or NOR4. R3 = H or acyl. R4 = H, acyl, alkyl or tetrahydropyranyl). They are prepd. e.g. from corresp. 3-oxo cpds. by reaction with an organometallic cpd. able to introduce R2 giving a tert. carbinol. (I) have powerful progestational activity and inhibit ovulation and implantation; the higher esters have delayed-release activity. The oral doses contain 0.01-0.5 mg and parenteral solns. about 100 mg/ml. In the Clauberg test 17 alpha-ethynyl-17 beta-hydroxy-18-methyl-4,15-oestradien-3-one is more active orally than the corresp. -4-oestren-3-one.