Methods of asymmetrically synthesizing enantiomers of casodex, its derivatives and intermediates thereof

摘要

Methods of synthesizing pure enantiomers of acylanalides such as Casodex(R) (bicalutamide) and its derivatives utilizing a compound having a ring structure that, when opened, provides a substituent having the structure of Formula I: wherein R¹ is alkyl or haloalkyl having up to 4 carbons; R² is alkyl having up to 6 carbon atoms; and R³ is CH₂OR⁴ where R⁴ is hydrogen or benzyl, C(O)CH₃, or C(O)OR⁵ where R⁵ is hydrogen or alkyl; are disclosed.