Abiraterone, CB-7598

阿比特龙Chemical Name: 17-(3-Pyridyl)androsta-5,16-dien-3beta-ol
CAS No. 154229-19-3
项目整合开发状态: Phase I
项目研究机构: BTG (Originator), Cougar Biotechnology (Licensee)
合成路线:Treatment of dehydroepiandrosterone 3-acetate (I) with triflic anhydride and 2,6-di-tert-butyl-4-methylpyridine provided the desired enol triflate (III) along with some 3,5-diene (II),which were separated by column chromatography.Subsequent coupling of triflate (III) with pyridylborane (IV) using bis(triphenylphosphine)- palladium(II) chloride as the catalyst afforded the (3-pyridyl)androstadiene (V),which after hydrolysis of the acetate ester with NaOH provided the target compound.