Shane Plunkett, Justin B. Diccianni, James Mulhearn, Soo Young Choi
) cross-coupling using alcohols as feedstocks have resulted in widespread adoption in analogue synthesis. Using high-throughput experimentation, an in situ alcohol activation with N-heterocyclic carbenes in DMA was discovered. Validation of the optimized, workup-free conditions suggested equivalent or greater reactivity to conditions where the alcohol is activated separately. The methodology was tested with a set of polar alcohols with drug-like properties, resulting in isolated product in 45/48 reactions.