Sterically demanding aryl–alkyl Suzuki–Miyaura coupling

Abstract

Efficient sterically demanding aryl–alkyl Suzuki–Miyaura coupling between di-ortho-substituted aryl halides and secondary alkylboronic acids has been achieved with a Pd-AntPhos catalyst that has shown high reactivity and a broad substrate scope with unprecedented steric hindrance. The methodology has facilitated the synthesis of molecular gears such as by cross-coupling.