Pd-catalyzed intermolecular consecutive double Heck reaction “on water” under air: facile synthesis of substituted indenes

An efficient and environmentally benign method for the preparation of substituted indene derivatives has been developed by using water as the sole solvent. This reaction proceeded under air, tolerated a wide range of functional-groups and was easily scaled up. Bioactive natural products like indriline were synthesized via the developed protocol. Preliminary results demonstrate that the enantioselective variant can also be achieved.