Ni Shengjun, Hribersek Matic, Baddigam Swarna K, Ingner Fredric J L, Orthaber Andreas, Gates Paul J, Pilarski Lukasz T
Department of Chemistry-BMC, Uppsala University, Box 576, 75123, Uppsala, Sweden.
Department of Chemistry-Ångström Laboratories, Uppsala University, Box 523, 75120, Uppsala, Sweden.
Angew Chem Int Ed Engl. 2021 Mar 15;60(12):6660-6666. doi: 10.1002/anie.202010202. Epub 2020 Dec 17.
The mechanochemical, solvent-free, highly regioselective, rhodium-catalyzed C-H methylation of (hetero)arenes is reported. The reaction shows excellent functional-group compatibility and is demonstrated to work for the late-stage C-H methylation of biologically active compounds. The method requires no external heating and benefits from considerably shorter reaction times than previous solution-based C-H methylation protocols. Additionally, the mechanochemical approach is shown to enable the efficient synthesis of organometallic complexes that are difficult to generate conventionally.
报道了铑催化的（杂）芳烃的机械化学、无溶剂、高区域选择性C-H甲基化反应。该反应具有出色的官能团兼容性，并已证明可用于生物活性化合物的后期C-H甲基化。该方法无需外部加热，且与以前基于溶液的C-H甲基化方案相比，反应时间大大缩短。此外，机械化学方法被证明能够有效合成传统方法难以生成的有机金属配合物。
