期刊
CHEMSUSCHEM
卷 12, 期 13, 页码 3064-3068出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cssc.201802919
关键词
dimethyl carbonate; late-stage modification; pharmaceutical; sodium metabisulfite; sulfonemethylation
A three-component cross-coupling protocol of boronic acid, sodium metabisulfite, and dimethyl carbonate was developed for the construction of significant functional methyl sulfones, in which introduction of sulfur dioxide at the last stage was successfully achieved in one step. Inorganic sodium metabisulfite was used as an eco-friendly sulfur dioxide source. Green dimethyl carbonate was employed as methyl reagent in this transformation. Diverse functional methyl sulfones were obtained from various readily available boronic acids. Notably, the last-stage modification of pharmaceuticals and the synthesis of Firocoxib were efficiently established through this strategy.
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