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

Runrun Li, Qiang Wei, Xin Wang, Zemei Ge, Runtao Li*

*State Key Laboratory of Nature and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, P. R. of China, Email:

R. Li, Q. Wei, X. Wang, Z. Ge, R. Li, Synthesis, 2017, 49, 4341-4349.

DOI: 10.1055/s-0036-1590803

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An efficient cascade reaction of diethyl 2-(ethoxymethyl­ene)malonate, different hydroxylamines and various amines provides ethyl 3-amino-5-oxoisoxazolidine-4-carboxylate derivatives, which are expected to be important in organic synthesis and medicinal chemistry.

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Key Words

isoxazolidines, 4-isoxazolines, cascade synthesis, amines, Michael addition

ID: J66-Y2017