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An efficient and versatile synthetic palladium‐catalyzed sp2 CH bond activation approach for the preparation of a series of C8‐benzyl xanthines has been developed using benzyl chlorides as coupling partners. The reactions take place rapidly in 1,4‐dioxane and proceed in the presence of [PdCl2(MeCN)2]/P(o‐tolyl)3 as a catalyst system and Cs2CO3 as a base to afford good to excellent yields of the corresponding C8‐benzylated xanthines of biological interest.
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Sahnoun et al. (2011) studied this question.
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