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METHOD FOR PREPARING ZYTIGA INTERMEDIATE

机译:ZYTIGA中间体的制备方法

摘要

Disclosed is a method for preparing a Zytiga intermediate. The intermediate is trifluoromethanesulfonate of dehydroepiandrosterone acetate and has a chemical structure represented by formula (II). In the method, dehydroepiandrosterone acetate and trifluoromethanesulfonic anhydride are subjected to sulfonylation reaction in a weak-base condition, and the weak-base condition is formed by at least one base of C1-C4 carboxylate of alkaline metal, C1-C4 carboxylate of alkaline-earth metal, oxalate of alkaline metal, oxalate of alkaline-earth metal, hydrophosphate of alkaline metal, hydrophosphate of alkaline-earth metal, fluoride of alkaline metal and fluoride of alkaline-earth metal. The present invention has advantages of environmental friendliness, mild reaction condition, simple operation and few side reactions, and facilitates industrialized mass production.
机译:公开了一种制备Zytiga中间体的方法。中间体是乙酸脱氢表雄酮的三氟甲磺酸盐,具有由式(II)表示的化学结构。在该方法中,使乙酸脱氢表雄酮和三氟甲磺酸酐在弱碱条件下进行磺酰化反应,并且弱碱条件由碱金属的C1-C4羧酸盐,碱金属的C1-C4羧酸盐中的至少一个碱形成。碱土金属的草酸盐,碱土金属的草酸盐,碱金属的氢磷酸盐,碱土金属的氢磷酸盐,碱金属的氟化物和碱土金属的氟化物。本发明具有环境友好,反应条件温和,操作简单,副反应少的优点,有利于工业化大规模生产。

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