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Photoinduced Decarboxylative Sulfonylation of Carboxylic Acids with Sodium Sulfinates
Weiya Kong1, Jiaxin Wang1, Chen Chen1
1Guangdong 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.
Abstract:
We report photoinduced decarboxylative sulfonylation of carboxylic acids with sodium sulfinates for synthesizing sulfones. The reaction proceeds under mild conditions, directly utilizing carboxylic acids without prefunctionalization, with copper acetate as the oxidant and sodium acetate as the base at room temperature. This method demonstrates excellent substrate compatibility, accommodating simple carboxylic acids, and drug molecules successfully converted into the corresponding sulfones. Furthermore, we developed a photoinduced two-step, one-pot protocol that integrated two carboxylic acids with DABSO (DABCO-bis(sulfur dioxide) adduct) to synthesize sulfones. Biological activity evaluation revealed that drug molecule-derived sulfones exhibited antiproliferative activity against tumor cells.
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