Ligand-free Suzuki coupling of arylboronic acids with methyl (E)-4-bromobut-2-enoate: synthesis of unconventional cores of HIV-1 protease inhibitors

Abstract

An effective ligand-free Suzuki coupling protocol to unite methyl (E)-4-bromobut-2-enoate with several arylboronic acids has been accomplished. Thus, a number of variously functionalized methyl 4-arylcrotonates have been achieved in high to excellent yields under mild conditions. This method enables the preparation of diverse aryl-substituted cores of HIV-1 protease inhibitors.