Enantioselective Synthesis of β-Fluoroamines from β-Amino Alcohols: Application to the Synthesis of LY503430

N,N-Dialkyl-beta-amino alcohols were enantiospecifically and regioselectively rearranged by using N,N-diethylaminosulfur trifluoride (DAST) to give optically active beta-fluoroamines in excellent yields and enantiomeric excesses. This rearrangement was applied to the enantioselective synthesis of LY503430, a potential therapeutic agent for Parkinson's disease.