C-S bond formation through nucleophilic substitution reaction of thiol derivatives with activated aryl halides.

A simple and milder reaction approach for the formation of C(sp2)-S(thiol) bonds through nucleophilic substitution (ipso mode) of activated aryl halides with aryl/alkyl thiols is reported. Good-to-excellent yields were achieved without any additives (viz. ligands or phase transfer catalysts). Higher yields were observed in the case of activated aryl fluorides relative to aryl chlorides and aryl bromides. This method is very useful in synthesizing pharmaceuticals and sulfur-based materials. The current approach is highly practical and widely adopted as it does not require the use of transition metal catalysts and work for different functional groups in ArX (X = F, Cl, and Br.).