| 摘要 |
The invention comprises compounds of the general formulae: <FORM:0965657/C1/1> wherein R is methyl or fluorine, R1 is hydrogen or methyl, R2 is hydrogen or a hydrocarbon carboxylic acyl group of less than 12 carbon atoms, R3 is hydrogen or an aliphatic hydrocarbon group of less than 9 carbons, R4 is hydrogen, an aliphatic hydrocarbon group of less than 9 carbons, an aryl group, an aralkyl group, a lower alkoxy or an aryloxy group of less than 13 carbons, R5 is hydrogen, fluorine, bromine or chlorine, X and X11 are hydrogen or fluorine, X1 is hydrogen or methyl, Y is keto or b -hydroxy, Z is a double bond or a saturated linkage between C6 and C7. The compounds are prepared by brominating a 2-hydroxymethylene-testosterone or its dihydroallo analogue, refluxing the resulting 2-bromo-2-aldehydo compound with methanolic sodium methoxide and condensing the 2a -bromo-3-keto compound produced with a thioformamide, thioacetamide, thiobutyramide, thiobenzamide, a -thiotoluamide, xanthogenamide, or a -phenoxythioacetamide in a solvent. If the starting material does not contain any nuclear unsaturation then bromination in acetic acid yields the 2a -bromo-3-keto compound directly. The invention is illustrated by twenty-nine detailed examples. U.S.A. Specification 2,908,693 is referred to. |
