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铜介导的芳基乙酸与亚硫酸钠的脱羧磺酰化反应。

Copper-Mediated Decarboxylative Sulfonylation of Arylacetic Acids with Sodium Sulfinates.

机构信息

Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, 1023 South Shatai Road, Baiyun District, Guangzhou 510515, People's Republic of China.

出版信息

Org Lett. 2020 Sep 18;22(18):7164-7168. doi: 10.1021/acs.orglett.0c02516. Epub 2020 Aug 27.

Abstract

Herein, we present a copper-mediated decarboxylative sulfonylation of arylacetic acids with sodium sulfinates that provides viable access to sulfone compounds. This protocol features readily available feedstocks, simple operations, high regioselectivities, and moderate to good yields. The newly obtained products could be converted to other useful compounds. Importantly, the products and their derivatives exhibited potent antitumor activities in vitro, which were tested by MTT assay.

摘要

本文报道了一种铜介导的芳基乙酸与亚磺酸钠的脱羧磺酰化反应,为合成砜类化合物提供了一种可行的方法。该方法具有原料易得、操作简单、区域选择性高、产率中等至良好等优点。新得到的产物可以转化为其他有用的化合物。重要的是,通过 MTT 测定法测试,这些产物及其衍生物在体外表现出很强的抗肿瘤活性。

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