Key Laboratory of Eco-Environment-Related Polymer Materials, Ministry of Education, College of Chemistry and Chemical Engineering, Northwest Normal University , Lanzhou, Gansu 730070, China.
J Org Chem. 2017 Oct 6;82(19):10628-10634. doi: 10.1021/acs.joc.7b01371. Epub 2017 Sep 14.
An efficient one-pot multistep strategy has been developed, comprising auto-oxidative difunctionalization of alkenes, oxidation of sulfides, and a further reduction of peroxides for the synthesis of complex β-hydroxysulfone derivatives from phenthiols and alkenes. This method has several advantageous characteristics, including readily available substrates, low-cost and environmental benign reagents, nontoxic and renewable solvents, and mild reaction conditions. The application of this transformation to the multigram-scale preparation of the anticancer drug bicalutamide is accomplished.
已经开发出一种高效的一锅多步策略，包括烯烃的自动氧化二官能化、硫化物的氧化和过氧化物的进一步还原，用于从苯硫酚和烯烃合成复杂的β-羟基砜衍生物。该方法具有几个优点，包括易得的底物、低成本和环境友好的试剂、无毒和可再生的溶剂以及温和的反应条件。该转化已应用于抗癌药物比卡鲁胺的多克规模制备。
