Synthesis of Potent Bicyclic Bisarylimidazole c-Jun N-Terminal Kinase Inhibitors by Catalytic C−H Bond Activation
- 23 December 2006
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of the American Chemical Society
- Vol. 129 (3) , 490-491
- https://doi.org/10.1021/ja0676004
Abstract
The efficient preparation of the privileged bicyclic bisarylimidazole kinase inhibitor scaffold was accomplished using rhodium-catalyzed C−H activation and intramolecular alkylation. The key C−H activation/alkylation step represents one of the first evaluations of diastereocontrol in catalyzed C−H activation/olefin alkylation processes. Several inhibitors of JNK3 were prepared using this sequence, with the most potent inhibitor having an IC50 value of 1.6 nM.Keywords
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