Synthesis of the anti-prostate cancer drug abiraterone acetate
Abiraterone acetate is used for the treatment of castration-resistant prostate cancer. Abiraterone acetate was synthesized from dehydroepiandrosterone via a three-step reaction including the formation of tosylhydrazone, cross-coupling reaction and acetylation, and a two-step purification including column chromatography and recrystallization with an overall yield of 51.9%. Here, an improved procedure for the preparation of abiraterone acetate is described. This synthetic process is of easy operation and low cost, which is suitable for industrialization.
Ma, Siyue,Li, Jianheng,Tang, Huayang,Xu, Feng
p. 461 - 469
(2018/03/27)
Synthesis method of abiraterone acetate
The invention discloses a synthesis method of abiraterone acetate. The method includes: taking dehydroepiandrosterone as the raw material, conducting condensation with p-toluenesulfonhydrazide, then carrying out coupling reaction with 3-bromopyridine, and conducting acetylation so as to synthesize the target product abiraterone acetate. According to the synthesis method provided by the invention, the route has mild reaction conditions, the raw materials are cheap and easily available, and the production cost is low.
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Paragraph 0023; 0024; 0031; 0032; 0039; 0040
(2017/09/02)
SYNTHESIS OF ABIRATERONE AND RELATED COMPOUNDS
The present invention relates to processes for obtaining abiraterone and derivatives thereof, such as abiraterone acetate, by means of a Suzuki coupling through a steroid borate of general formula (IV) or a C—C coupling through a steroid hydrazone of general formula (II), as well as to intermediates useful in said processes.
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Paragraph 0201; 0202; 0203
(2014/02/15)
SYNTHESIS OF ABIRATERONE AND RELATED COMPOUNDS
The present invention relates to processesfor obtaining abirateroneand derivatives thereof, such as abiraterone acetate, by means of a Suzuki coupling through a steroid borate of general formula (IV) or a C-C coupling through a steroid hydrazone of general formula (II), as well as to intermediates useful in said processes.
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Page/Page column 32
(2013/03/28)
Processes for the preparation of abiraterone and related compouds
The present invention relates to processes for obtaining abiraterone and derivatives thereof, such as abiraterone acetate, by means of a C-C coupling through a steroid hydrazone of general formula (II) or a Suzuki coupling through a steroid borate of general formula (IV), as well as to intermediates useful in said processes.
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Paragraph 0088; 0089; 0090
(2013/07/19)
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