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Convenient, practical and economical phosphorylation of thiols has been achieved via halogen- and metal-free K2CO3-promoted aerobic oxidative cross-coupling of trialkyl phosphites, dimethyl phenylphosphonite, or methyl diphenylphosphinite with thiophenols using air as the oxidant at room temperature. This transformation provides a straightforward route to the construction of phosphorus–sulfur bonds with wide functional group compatibility, which affords phosphorothioates in up to 94% yield.

Graphical abstract: K2CO3-promoted aerobic oxidative cross-coupling of trialkyl phosphites with thiophenols

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