Abstract

AbstractA P(NMe2)3‐mediated reductive (1+4) annulation reaction of α‐keto esters with substituted nitroalkenes has been developed, providing a feasible protocol to construct polysubstituted isoxazoline N‐oxides in moderate to excellent yields from readily available starting materials. This reaction originates from the characteristic reactivity of in situ generated Kukhtin‐Ramirez adducts and presumably proceeds through a tandem Michael addition‐intramolecular SN2 sequence. To further expand the utility of this annulation reaction, isoxazolines have been efficiently prepared from corresponding annulation products upon treatment with trimethyl phosphite.

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