Synthesis of 4-amino-2-trifluormethyl quinoline derivatives via palladium-catalyzed cascade reactions of isocyanides with N-(ortho-iodo)aryl enamines

•A novel approach to 4-amino-2-trifluormethylquinoline derivatives is described.•Isocyanides as a C1 building blocks were used to construct heterocycles.•The target heterocycles can be found in many natural products or drugs.

A novel efficient synthetic approach to 4-amino-2-trifluormethyl quinoline derivatives is described via palladium-catalyzed cascade reactions of isocyanides with readily available N-(ortho-iodo)aryl enamines under mild conditions. The target heterocycles can be found in many natural products or drugs, which were obtained in generally good to excellent yield.

Graphical abstractA novel efficient synthetic approach to 4-amino-2-trifluormethyl quinoline derivatives is described via palladium-catalyzed cascade reactions of isocyanides with readily available N-(ortho-iodo)aryl enamines under mild conditions. The target heterocycles can be found in many natural products or drugs, which were obtained in generally good to excellent yield.Figure optionsDownload full-size imageDownload as PowerPoint slide