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1,2-Azaborines, a unique class of BN-isosteres of benzene, have attracted great interest across several fields. While significant advancements have been made in the postfunctionalization of 1,2-azaborines, challenges still exist for the selective functionalization of the C4 position and access to 1,2-azaborines with five or six independently installed substituents. Here we report a rapid and modular method for C3 and C4 difunctionalization of 1,2-azaborines using the palladium/norbornene (Pd/NBE) cooperative catalysis. Enabled by the C2 amide-substituted NBE, diverse 3-iodo-1,2-azaborines can be used as substrates, showing broad functional group tolerance. Besides
Choi et al. (2024) studied this question.