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. Author manuscript; available in PMC: 2019 Jun 14.
Published in final edited form as: J Med Chem. 2018 May 24;61(11):4946–4960. doi: 10.1021/acs.jmedchem.8b00419

Scheme 1. Synthesis of abiraterone and its derivativesa.

Scheme 1.

aReagents and conditions: (a) phenylboronic acid, Pd(PPh3)2Cl2, NaHCO3, THF, H2O, 60 °C, 23 h, 70%; (b) K2CO3, MeOH, rt, 17 h, 93%; (c) diethyl(3-pyridyl)borane, Pd(PPh3)2Cl2, NaHCO3, THF, H2O, 60 °C, 23 h, 77%; (d) K2CO3, MeOH, rt, 16 h, 62% (e) Al(O-i-Pr)3, 2-butanone, toluene, reflux, 20 h, 60%