| 摘要 |
The invention comprises compounds of formula <FORM:0984028/C2/1> where R1 is an alkyl radical having 1-4 carbon atoms or a benzyl radical, R2 is an alkyl radical having 1 to 4 carbon atoms, R3 is a hydrogen atom, an alkyl radical having 1 to 4 carbon atoms, or a vinyl, allyl or ethynyl radical, and n is an integer from 2 to 5 inclusive, acid addition salts thereof, and their preparation by (a) reacting an estradiol of formula <FORM:0984028/C2/2> with an aminoalkyl halide of formula R1R2N-(CH2)n-X wherein X is a halogen atom, in the presence of a base, or (b) reducing on estrone of formula <FORM:0984028/C2/3> (prepared as described in Specification 984,029). The compounds of the invention are anti-fertility and hypocholesteremic agents and pituitary inhibitors, and may be used alone or in combination with one or more pharmaceutical diluents or excipients, e.g. as tablets, pills, sachets and packaged or encapsulated powders. Specification 984,030 also is referred to. |
