An Efficient Cascade Synthesis of Ethyl 3-Amino-5-oxoisoxazolidine-4-carboxylate Derivatives

An efficient cascade synthesis of ethyl 3-amino-5-oxoisoxazolidine-4-carboxylate derivatives from diethyl 2-(ethoxymethylene) malonate, different hydroxylamines and various amines is developed. This approach tolerates a wide range of amines affording highly functionalized isoxazolidine derivatives, which are expected to be important in organic synthesis and medicinal chemistry.