Aromatic azaheterocycles are ubiquitous components of bioactive small molecules, with over 250 FDA-approved treatments containing these motifs. New approaches that allow for the direct and selective modification of these structures—without the inclusion of any additional directing groups—would allow for straightforward access to desirable chemical space. Here, we describe our approach to selective C-H functionalization that takes advantage of simultaneous Lewis acid catalysis and organic hydrogen atom transfer catalysis. This dual catalytic strategy delivers highly site-selective formation of new C-N, C=O, and C-F bonds.

Dual catalysis strategies for site selective functionalization of azaheterocycles

255th National Meeting (2018)

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