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.

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In this work, we report the strategy of one-pot synthesis of protoberberine alkaloid derivatives via palladiumcatalyzed cascade α-arylation and cyclization, which can afford the target molecules in moderate to excellent isolated yields using commercially available raw materials under solvent-free conditions. This protocol provides an efficient and convenient path to multisubstituted protoberberine derivatives. In addition, it can directly afford natural alkaloids.

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