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Abstract

A method for preparing abiraterone acetate. The steps are: dehydroepiandrosterone acetate and trifluoromethanesulphonic anhydride undergo a sulfonylation reaction under the catalysis of an organic base to obtain a compound as represented by formula II; the compound is reacted with a 3-pyridine organoboron compound or a 3-pyridine organosilicone compound under the catalysis of Bis(triphenylphosphine) palladium(II) dichloride to obtain a crude abiraterone acetate product; the crude product is recrystallized in a protic or aprotic solvent to obtain an abiraterone acetate crystal; the crystal is further put into a solvent which easily dissolves the crystal and dissolved under heating, and the solution is dropwise added into a solvent which does not easily dissolve the crystal until a solid is precipitated under stirring, such that a micro powder abiraterone acetate is obtained; and the solvent which easily dissolves the crystal is a mixture of any two or more of acetone, ethanol and water, and the solvent which does not easily dissolve the crystal is water. The method has a rational route, a simple and convenient operation, a good product quality, and a high yield. No column chromatography, and salt-formation are required in the entire process to satisfy requirements of industrial scale productions. Furthermore, an abiraterone acetate particle size of about 10 um is obtained.

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