化学
双环分子
烷基化
烯烃纤维
分子内力
催化作用
立体化学
组合化学
铑
有机化学
作者
Jason C. Rech,Michihisa Yato,Derek R. Duckett,Brian Ember,Philip V. LoGrasso,Robert G. Bergman,Jonathan A. Ellman
摘要
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.
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