Synthesis of 4-sulfonyl-1,7-diesters via K 2 CO 3 -mediated alkylative debenzoylation of α-sulfonyl o -hydroxyacetophenones with acrylates.

The synthesis of 4-sulfonyl-1,7-diesters was well developed, under open-vessel conditions, by K 2 CO 3 -mediated double alkylation of α-sulfonyl o -hydroxyacetophenones with acrylates and tandem debenzoylation of the resulting α,α-disubstituted o -hydroxyacetophenones. A plausible mechanism is proposed and discussed here. This high-yielding protocol provides a highly effective intermolecular alkylation and intramolecular debenzoylation via the formation of two carbon-carbon (C-C) single bonds and the cleavage of a carbon-carbon (C-C) single bond.