State Key Laboratory of Elemento-Organic Chemistry, College of Chemistry, College of Pharmacy, Frontiers Science Center for New Organic Matter, Nankai University, Tianjin 300071, People's Republic of China.
Tianjin Yugen Medtech Co., Tianjin 30457, People's Republic of China.
Org Lett. 2022 Mar 18;24(10):2064-2068. doi: 10.1021/acs.orglett.2c00722. Epub 2022 Mar 8.
A mild method for the deborylation deuteration of arylboronic acids with DO, mediated by the synergistic combination of a thiol, a Lewis base, and photoredox catalysis, is reported. This reaction showed a broad substrate scope, excellent deuterium incorporation, and functional group tolerance. Therefore, this method is practical for the site-selective D-labeling of bioactive molecules and drug molecules.
本文报道了一种温和的芳基硼酸去硼氘代方法，该方法使用 DO 作为氘源，通过硫醇、路易斯碱和光氧化还原催化的协同组合进行介导。该反应具有广泛的底物范围、优异的氘掺入和官能团耐受性。因此，该方法可用于生物活性分子和药物分子的位点选择性 D 标记。
