Catalyst-free synthesis of 3-(1-arylsulfonylalkyl)indoles via three-component reaction of indoles, carbonyls, and arenesulfinic acids

ABSTRACT

A catalyst-free three-component reaction of indoles, carbonyls, and arenesulfinic acids performed at room temperature provides direct access to biologically important 3-(1-arylsulfonylalkyl)indoles. This process features mild conditions, low cost, broad substrate scope, and high yields, and mechanistically bis(indolyl)methanes were identified as the key intermediates.

GRAPHICAL ABSTRACT

KEYWORDS:

• Multicomponent reaction
• Indole functionalization
• sulfinic acids

Funding

Financial support for this research by the Applied Basic Research Programs of Yunnan Science and Technology Department (2014FD039 and 2013FZ103), the General Projects of Yunnan Education Department (2013Y252), and the Students Research Projects of Kunming University (XJD15079) is gratefully acknowledged.