Treatment of (+/-)-2-phenyl-4-tert-butyloxazolin-5(4H)-8 with Lipozyme(R) (Mucor miehei) in toluene containing n-butanol and a catalytic amount of triethylamine resulted in a 94% yield of (S)-N-benzoyl tert-leucine butyl ester 9 (99.5% e.e.). Subsequent two step hydrolysis (Alcalase(R) followed by 6N HCl, reflux) yielded homochiral L-(S)-tert-leucine 1.