Rapid and selective access to three distinct sets of indole-based heterocycles from a single set of Ugi-adducts under microwave heating

摘要

Three distinct sets of indole-based heterocycles were rapidly and selectively synthesized from the same set of Ugi-adducts under microwave heating in a reaction-condition-controlled manner. Notably, an unprecedented metal-free intramolecular sp~3-hybridized C-H arylation using only cesium carbonate was discovered. Rapid access to molecular complexity and diversity from simple starting materials is particularly useful in organic synthesis and drug discovery. Multi-component reactions (MCRs) provide a powerful complexity-generating approach to easily transform three or more starting materials into a single product in an atom- and step-economical way.