Department of Chemistry, Renmin University of China, Beijing 100872, China.
J Org Chem. 2021 Mar 5;86(5):3981-3988. doi: 10.1021/acs.joc.0c02827. Epub 2021 Feb 16.
The budding deuteriodifluoromethyl group (CFD) is a potentially significant functional group in medicinal chemistry. Herein, we investigated -BuOK-catalyzed H/D exchange reaction of difluoromethylarenes in DMSO- solution. The method provides excellent deuterium incorporation at the difluoromethyl group. Meanwhile, the effect of a trace amount of DO in DMSO- solution on the deuteration reaction was also investigated.
潜在的重要的官能团在药物化学中的萌芽氘代二氟甲基基团(CFD)。在此,我们研究了 -BuOK 催化的二氟甲基芳烃在 DMSO-溶液中的 H/D 交换反应。该方法在二氟甲基上提供了极好的氘取代。同时,还研究了 DMSO-溶液中痕量 DO 对氘代反应的影响。