Synthesis of Potent Bicyclic Bisarylimidazole c-Jun N-Terminal Kinase Inhibitors by Catalytic C-H Bond Activation

摘要

The privileged bisarylimidazole framework is found in a variety of potent kinase inhibitors,some of which have entered clinical trials.Bicyclic bisarylimidazole derivatives,such as the c-jun N-terminal kinase 3 (JNK3) inhibitor 1 (Figure 1),have recently been developed to enhance affinity and particularly selectivity,which remains a key challenge in kinase inhibitor drug discovery efforts.