A cascade reaction for regioselective construction of pyrazole-containing aliphatic sulfonyl fluorides

A copper-catalyzed cascade reaction of α-diazocarbonyl compounds with ethenesulfonyl fluoride (ESF) is developed, affording a variety of highly functionalized pyrazolyl aliphatic sulfonyl fluorides in good to excellent yields (66-98%). This transformation features broad substrates, exclusive regioselectivity, high atom economy and operational simplicity, thus providing a straightforward method for the direct construction of pyrazole-containing aliphatic sulfonyl fluorides, which will provide great applicable value in medicinal chemistry and other related disciplines. A copper-catalyzed cascade reaction of α-diazocarbonyl compounds with ethenesulfonyl fluoride for the construction of pyrazole-containing aliphatic sulfonyl fluorides is developed.