Microwave Irradiation as a High-Speed Tool for Activation of Sluggish Aryl Chlorides in Grignard Reactions

Grignard reagents have been generated from reluctant aryl chlorides and bromides using controlled microwave heating to establish a safe, productive and reproducible method. In the synthesis of a novel HIV-1 protease inhibitor, microwave irradiation was both used to generate the starting arylmagnesium halide and to promote a subsequent Kumada coupling.