Abstract

A novel and straightforward procedure for the synthesis of thioester-substituted indolo[2,1-a]isoquinolines has been established. The reaction proceed via nickel-catalyzed cyclization/thiocarbonylation from alkene-tethered indoles and sulfonyl chlorides. Very good compatibility toward a wide range of functional groups was observed, both aryl and alkyl sulfonyl chlorides were well tolerated. With Mo(CO)6 as a convenient and solid CO surrogate, and by using sulfonyl chloride as an abundant and cheap sulfur source, a variety of thioester-substituted indolo[2,1-a]isoquinolines were obtained in moderate to high yields.

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