Environmentally benign protocol for the direct amination of bromo- and iodoarenes using a Cu catalyst.
Simple and efficient CuI/PEG-400 system for amination of aryl halides with aqueous ammonia
This paper by Chen (Jiangxi Normal University, China) seems really more suitable for Process Development than Drug Discovery, but I think it is interesting anyway. Besides the efforts of some researchers (Buchwald, for example) to stablish a universal direct amination protocol using ammonia and a Palladium catalyst, other people is trying with another catalysts. Here the metal is Copper, and the substrates are bromo- and iodoarenes. The method looks quite green, using water and PEG as reaction medium, with CuI as catalyst. 27 examples are described, though as usual the ortho substrates are avoided. Maybe the use of MW can accelerate the reaction; water is not exactly the best solvent for that, but since you have also the PEG and salts in the medium I think trying it is worth.
Tetrahedron Lett. 2011, 52 (29), pages 3710-3713. See: 10.1016/j.tetlet.2011.02.096
