Synthesis of Isoxazoles via One-Pot Oxidation/Cyclization Sequence from Propargylamines

A facile strategy for the synthesis of isoxazoles has been efficaciously developed, which involves oxidation of propargylamines to the corresponding oximes followed by CuCl-mediated intramolecular cyclization of the latter. This protocol shows a straightforward way to construct a series of isoxazole cores with a wide range of functional group compatibility. Meanwhile, a gram-scale experiment and synthetic applications can be successfully operated.

Automated summary

A facile strategy for synthesis of isoxazoles involving oxidation of propargylamines to oximes followed by CuCl-mediated cyclization has been developed. This protocol allows for construction of isoxazole cores with wide functional group compatibility, and can be successfully scaled up for gram-scale experiments and synthetic applications.