{"title":"Palladium-Catalyzed Site-Selective C–H Sulfonylation via Aryl Thianthrenium Salts to Access Diarylsulfones","authors":"Chunjie Ni, Jin-Ping Liu, Xiao-Xu Zhang, Zi-Yi Wang, Zhanhang Liang, Chen Chen, Di Qiu","doi":"10.1021/acs.joc.4c02913","DOIUrl":null,"url":null,"abstract":"We presented a highly efficient palladium-catalyzed site-selective C–H sulfonylation reaction via aryl thianthrenium salts. By utilizing readily available and cost-effective arenes along with sodium sulfinates, we achieved the C(sp<sup>2</sup>)–S cross-coupling with high efficiency, establishing a dependable method for synthesizing diarylsulfones with satisfactory yields. This method exhibits excellent tolerance toward functional groups, scalability, and the synthesis or late-stage functionalization of bioactive molecules, making it a valuable sulfonylation tool for drug modifications.","PeriodicalId":57,"journal":{"name":"Journal of Organic Chemistry","volume":"25 1","pages":""},"PeriodicalIF":3.3000,"publicationDate":"2025-02-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Organic Chemistry","FirstCategoryId":"1","ListUrlMain":"https://doi.org/10.1021/acs.joc.4c02913","RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"CHEMISTRY, ORGANIC","Score":null,"Total":0}
引用次数: 0
Abstract
We presented a highly efficient palladium-catalyzed site-selective C–H sulfonylation reaction via aryl thianthrenium salts. By utilizing readily available and cost-effective arenes along with sodium sulfinates, we achieved the C(sp2)–S cross-coupling with high efficiency, establishing a dependable method for synthesizing diarylsulfones with satisfactory yields. This method exhibits excellent tolerance toward functional groups, scalability, and the synthesis or late-stage functionalization of bioactive molecules, making it a valuable sulfonylation tool for drug modifications.
期刊介绍：
Journal of Organic Chemistry welcomes original contributions of fundamental research in all branches of the theory and practice of organic chemistry. In selecting manuscripts for publication, the editors place emphasis on the quality and novelty of the work, as well as the breadth of interest to the organic chemistry community.
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