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The benzofuran skeleton is commonly found in a wide variety of natural products that display a wide range of biological activities.For this reason, benzofuran has a high potential for use as a scaffold in both chemical and pharmaceutical syntheses of natural products.This work describes the development of a novel asymmetric synthetic method of benzofuran-derived β-amino esters via K2CO3-catalyzed domino reactions of ortho-hydroxyl aromatic N-tert-butylsulfinyl imines and diethyl bromomalonate.A small library of target compounds was prepared under optimized reaction conditions in moderate to good yields with high distereoselective and enantioselective properties.The newly-generated chiral carbon-center was of an (S)-configuration as determined by X-ray diffraction.