114212-24-7Relevant articles and documents
Enantioselective (3+2) cycloaddition: Via N-heterocyclic carbene-catalyzed addition of homoenolates to cyclic N -sulfonyl trifluoromethylated ketimines: Synthesis of fused N-heterocycle γ-lactams
Zhang, Zhen-Zhen,Zhang, Yongna,Duan, Hui-Xin,Deng, Zhuo-Fei,Wang, You-Qing
supporting information, p. 1553 - 1556 (2020/02/13)
An enantioselective (3+2) cycloaddition of enals and cyclic N-sulfonyl trifluoromethyl ketimines via N-heterocyclic carbene-catalyzed homoenolate addition is described. This reaction can efficiently construct fused N-heterocycle γ-lactams bearing two adjacent chiral centers with >20?:?1 dr and 94-99% ee, with one chiral center as a trifluoromethylated α-tetrasubstituted carbon stereocenter.
Synthetic and computational studies on liphagal: A natural product inhibitor of PI-3K
Zhang, Yanzhong,Oblak, E. Zachary,Bolstad, Erin S.D.,Anderson, Amy C.,Jasinski, Jerry P.,Butcher, Ray J.,Wright, Dennis L.
experimental part, p. 6120 - 6122 (2010/12/24)
The natural product liphagal has been shown to function as a reasonably potent and selective inhibitor of the key signaling enzyme PI-3Kα. We have been interested in developing an analog class of PI-3K inhibitors based upon this unusual terpenoid natural product. Toward that end, we have evaluated the binding of the natural product to its target protein computationally and formulated a class of simplified analogs based on the structural analysis. Utilizing the cycloadduct derived from tetrabromocyclopropene and furan, we were able to generate a key, versatile scaffold upon which to pursue this analog design.
