A rapid construction of 1,3,2-benzodiazaborininones [R-B(aam)] from boronic acids and anthranilamides.

A simple, efficient and mild methodology for the synthesis of 1,3,2-benzodiazaborininones [R-B(aam)] from boronic acids and anthranilamides on ethyl acetate is described. A series of 1,3,2-benzodiazaborininones were prepared in moderate to excellent yields at room temperature without dehydrating agents, metal catalysts, corrosive acids or other additives. Meanwhile, a multi-gram scale reaction is also performed to ensure the scalability of the reaction, and the product can be conveniently isolated by simple filtration.