10 displacement 4 estrene chemical compound

摘要

NEW MATERIAL:A compound of formula I [R is hydroxymethyl, difluoromethyl, formyl, 2-4C alkanoyloxymethyl; X is oxo, formula II (R1 is 2-4C alkanoyl)]. EXAMPLE:19-Hydroxy-4-androsten-17-one. USE:Inhibitor of estrogen biosynthesis. PREPARATION:For example, in case that R is hydroxymethyl, 1 mole of a compound of formula III (X1 is oxo, formula II) and 1 to 1.2 mole of an alkane dithiol of formula IV (A is 2-4C alkylene) are allowed to react with each other in a solvent such as acetic acid or benzene in the presence of 0.05 to 0.5 mole of a condensing agent such as p-toluenesulfonic acid at about 0 to 100 deg.C to give a compound of formula IV. Then, the product is reduced with liquid ammonia and metallic sodium or the like in a solvent such as THF to give the compound of formula I.