State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Xue Yuan Rd. 38, Beijing, 100191, China.
State Key Laboratory of Organometallic Chemistry, Chinese Academy of Sciences, Shanghai, 200032, China.
Angew Chem Int Ed Engl. 2017 Feb 20;56(9):2487-2491. doi: 10.1002/anie.201612190. Epub 2017 Jan 23.
An efficient Cs CO -catalyzed oxidative coupling of thiols with phosphonates and arenes that uses molecular oxygen as the oxidant is described. These reactions provide not only a novel alkali metal salt catalyzed aerobic oxidation, but also an efficient approach to thiophosphates and sulfenylarenes, which are ubiquitously found in pharmaceuticals and pesticides. The reaction proceeds under simple and mild reaction conditions, tolerates a wide range of functional groups, and is applicable to the late-stage synthesis and modification of bioactive molecules.
本文描述了一种高效的 Cs CO 催化的硫醇与膦酸酯和芳基的氧化偶联反应,该反应以分子氧作为氧化剂。这些反应不仅提供了一种新的碱金属盐催化的有氧氧化,而且还提供了一种高效的合成硫代磷酸酯和亚磺酰芳基的方法,这些化合物在药物和农药中广泛存在。该反应在简单温和的反应条件下进行,能够容忍广泛的官能团,并且适用于生物活性分子的后期合成和修饰。