Similar results were observed in the asymmetric benzylation reaction. Various substituted benzyl chlorides exhibited good activities in this reaction and gave the corresponding products in moderate-to-high yields with goodto-excellent enantioselectivities (Figure , 9b-9j). When the methyl 2-(chloromethyl)benzoate 8b was used as an acceptor, the product 9k was obtained in 52% yield with 92% ee via a tandem benzylation/lactamization process. Because of the steric influence of their substituents, amino acid esters other than 1a products with moderate yields. In addition, all the enantioselectivities for these products were maintained at a high level 6, 9l-9r). The absolute configurations of products 6b (S) and 9a (S) were determined by comparing their optical rotation values with the literature data (see Supporting Information), and the stereochemistries of the other products in Figure were assigned accordingly.