| 摘要 |
PURPOSE:To obtain the titled compound useful as an intermediate for pharmaceuticals, in high yield, by mixing an aqueous solution of hydrochloric acid to a reaction mixture of an acyloxy-estratrien-ol with a monohalogenoacetyl halide and separating the produced crystal by filtration. CONSTITUTION:A 3-acyloxy-1,3,5(10)-estratrien-17beta-ol of formula I (R is acyl) is made to react with a monohalogenoacetyl halide (preferably monobromoacetyl bromide) in a solvent (e.g. THF) using pyridine as a catalyst preferably at 0-10 deg.C. The obtained reaction liquid is mixed with an aqueous solution of hydrochloric acid and produced crystal is separated by filtration to obtain the objective compound of formula II (X is halogen). The amount of the monohalogenoacetyl halide is preferably 1.05-2.00mol. per 1mol. of the compound of formula I.
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