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METHOD FOR PREPARING ZYTIGA INTERMEDIATE
METHOD FOR PREPARING ZYTIGA INTERMEDIATE
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机译:ZYTIGA中间体的制备方法
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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.
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