One-Pot Synthesis of β-Hydroxysulfones and Its Application in the Preparation of Anticancer Drug Bicalutamide,The Journal of Organic Chemistry

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One-Pot Synthesis of β-Hydroxysulfones and Its Application in the Preparation of Anticancer Drug Bicalutamide
The Journal of Organic Chemistry ( IF 3.3 ) Pub Date : 2017-09-14 00:00:00 , DOI: 10.1021/acs.joc.7b01371
Yajun Wang ₁ , Wei Jiang ₁ , Congde Huo ₁

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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.

中文翻译：

一锅法合成β-羟基砜及其在制备抗癌药物比卡鲁胺中的应用

已经开发了一种有效的一锅多步策略，包括烯烃的自氧化双官能化，硫化物的氧化以及过氧化物的进一步还原，用于由苯硫酚和烯烃合成复杂的β-羟基砜衍生物。该方法具有几个有利的特征，包括容易获得的底物，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。完成了该转化在抗癌药物比卡鲁胺的克级制备中的应用。

更新日期：2017-09-15

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