| 摘要 |
1,145,336. 17α - Furyl - strogens. AYERST, McKENNA & HARRISON Ltd. 8 June, 1966 [14 Sept., 1965], No. 25574/66. Heading C2U. The invention comprises compounds of formula wherein R is a hydrogen atom or a C 2-4 -aliphatic acyl group and R<SP>1</SP> is a hydrogen atom or a C 1-4 alkyl, C 5-6 cycloalkyl, 2-tetrahydropyranyl or acyl group or a group -SO 3 <SP>-</SP>X<SP>+</SP>, wherein X is a sodium, potassium, calcium, magnesium, barium, ammonium or organic base cation, the dotted lines indicating one optional 7(8) double bond or two optional 6(7) and 8(9) double bonds, and their preparation by reaction of 3-furyllithium with a compound of formula wherein R<SP>1</SP> is a hydrogen atom or a C 1-4 alkyl, C 5-6 cycloalkyl or 2-tetrahydropyranyl group, followed, if desired, by (a) 3 and/or 17-etherification or esterification or (b) reaction of a 3-ol with chlorosulphonic acid in the presence of an organic base, with optional conversion to an ammonium or inorganic salt. 3-(C 2-4 alkyl and C 5-6 cycloalkyl) ethers of equilin and equilenin are prepared by reaction of a sodium or potassium salt of the steroid with an alkyl or cycloalkyl halide. The compounds of the invention have estrogenic activity and may be used in pharmaceutical compositions in combination with a carrier, for example in forms suitable for oral or parenteral administration. |
