Copper-catalysed direct C-H bond sulfonylation of aminoquinolines using commercially available and inexpensive arylsulfonyl chlorides as the sulfonylation reagents is described. The reactions took place exclusively at the C5-H position of the quinoline rings and tolerated a wide spectrum of functional groups. Moreover, synthetic transformations of the sulfonylated products led to useful compounds.

Copper-catalyzed direct C-H bond sulfonylation of aminoquinolines with arylsulfonyl chlorides leads to useful compounds with a wide range of functional groups.

Paper

Selective remote C-H sulfonylation of aminoquinolines with arylsulfonyl chlorides via copper catalysis.

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