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Pd-Catalyzed C(sp3)–H Biarylation via Transient Directing Group Strategy

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journal contribution
posted on 18.09.2020, 21:55 by Mingruo Ding, Wenkai Hua, Min Liu, Fengzhi Zhang
Here, we describe a highly selective Pd-catalyzed C­(sp3)–H biarylation of 2-methylbenzaldehydes using cyclic diaryliodonium salts as arylation reagents. The key strategy is the employment of tert-leucine as a bidentate transient directing group for the proximity-driven metalation to achieve reactivity and selectivity in C–H activation. Various functionalized biaryls bearing both aldehyde and iodine functional groups were prepared successfully, which could be further transformed into a wide range of compounds with potential applications in pharmaceutical chemistry and materials science.