Abstract
| - The palladium-catalyzed, two-step, one-pot borylation/Suzuki coupling (BSC) reaction was developedto synthesize sterically hindered 2,2‘-disubstituted biphenyl and phenyl-indole compounds in a short,simple, and efficient manner from two easily accessible aryl halides. High yields can be obtainedby choosing properly both components according to their rough electronic properties. The illustrationof the utility of this method was provided by the solution and solid-phase synthesis of seven- oreight-membered biphenyl lactams 5a−e, as well as paullone 3a. These compounds exhibit moderatealbeit significant cytotoxicities and may serve as structural models for future medicinal chemistrydevelopments.
|