Methods of synthesizing pure enantiomers of acylanalides such as Casodex (bicalutamide) and its derivatives utilizing a compound having a ring structure that, when opened, provides a substituent having the structure of Formula I: ##STR1##

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.

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