The Asymmetric Arylation Reaction. After determining the optimal reaction conditions, we examined the substrate scopes for this reaction. First, various substituted amino acid esters were employed as reaction partners with 2-nitro fluorobenzene 2a (Figure ). The variation of the alkoxyl group on reactant 1 affected the yields but had little influence on the enantioselectivity (Figure ). Generally, the benzyl and methyl alaninate produced corresponding products 3c and 3e in moderate yields. The decrease in yields may be caused by the amine-ester exchange reaction of amino acid esters containing less bulky alkoxyl groups. Amino acid esters bearing saturated linear alkyls were effective reaction partners for 2a, producing 3f-3i in good-to-high yields with excellent enantioselectivities. Similar results were observed when the saturated branched alkyl-or unsaturated linear alkylsubstituted amino acid esters participated in this reaction (Figure ). Other functional groups, such as ester, sulfoxide, and indolyl, that are contained in the amino acid esters were well tolerated under the optimal reaction conditions; products 3n-3q were obtained in moderate-togood yields with excellent enantioselectivities. The model reaction was readily expanded to the gram scale. With 10 mmol of 2-nitro fluorobenzene, compound 3a was produced in 74% yield (1.97 g) with > 99% ee.