The aminopyridine (2 -Figure ) is a well-described molecular scaffold that has been shown to accommodate the folded P-loop conformation in MAP4K4. Additionally, this scaffold is small and versatile, allowing the attachment of different substituents on both sides of the aminopyridine core by a short synthetic route. The co-crystal structures of VRK1 and VRK2 bound to 1 (BI-D1870) also revealed that the ligand difluorophenol moiety facilitated favorable polar interactions to catalytically-important residues within the VRK ATP-binding site. Thus, our design strategy to develop new small molecule inhibitors for VRK1 and VRK2 was to hybridize the aminopyridine core with the difluorophenol group. Synthesis of the aminopyridine derivatives was performed using a rapid and efficient two-step Suzuki-Miyaura coupling (Figure ) with yields ranging between 18% and 89%. Each step was performed by a microwave-assisted reaction in one hour. Details of the procedure are available in the Supporting Information.