A copper-mediated
decarboxylative coupling reaction of 3-indoleacetic
acids with pyrazolones was described. This protocol realized new functionalization
of pyrazolones under simple reaction conditions and exhibited high
functional group compatibility and broad substrate scope. Notably,
the products displayed antiproliferative activity against cancer cells.
Herein, we present a copper-mediated decarboxylative sulfonylation of arylacetic acids with sodium sulfinates that provides viable access to sulfone compounds. This protocol features readily available feedstocks, simple operations, high regioselectivities, and moderate to good yields. The newly obtained products could be converted to other useful compounds. Importantly, the products and their derivatives exhibited potent antitumor activities in vitro, which were tested by MTT assay.
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