A novel asymmetric synthetic strategy to prepare 4-aryl-dihydroisoquinolinones has been developed through a highly regioselective Friedel-Crafts alkylation of benzylamine derivatives with (αR)-α-bromo arylacetates and subsequent facile lactamization. In addition, an efficient asymmetric synthesis of 2-aryl morpholinones is demonstrated with 2-aminoethanol derivatives using the same convenient substitution-lactamization protocol.

中文翻译：

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AgOTf活化的α-溴代芳基乙酸酯不对称合成4-芳基二氢异喹啉-3-酮和2-芳基吗啉-3-酮

通过用（αR）-α-溴代芳基乙酸酯对苄胺衍生物进行高度区域选择性的Friedel-Crafts烷基化反应，并随后进行轻松的内酰胺化反应，已开发出制备4-芳基-二氢异喹啉酮的新型不对称合成策略。另外，使用相同的方便取代-内酰胺化方案，证明了2-氨基乙醇衍生物能有效地不对称合成2-芳基吗啉酮。