A5077984600- Catalytic C–H Functionalization Methods
- Catalytic Cross-Coupling Reactions
- Synthesis and Catalytic Reactions
- Asymmetric Hydrogenation and Catalysis
- Synthesis and biological activity
- Melanoma and MAPK Pathways
- Asymmetric Synthesis and Catalysis
- Radical Photochemical Reactions
- Synthetic Organic Chemistry Methods
- PI3K/AKT/mTOR signaling in cancer
- Cyclopropane Reaction Mechanisms
China Pharmaceutical University
2019-2020
Abstract Transition-metal-catalyzed tandem Heck/carbonylation reaction has emerged as a powerful tool for the synthesis of structurally diverse carbonyl molecules, well natural products and pharmaceuticals. However, asymmetric version was rarely reported, remains challenging topic. Herein, we describe palladium-catalyzed desymmetrization cyclopentenes. Alcohols, phenols amines are employed versatile coupling reagents construction multifunctional chiral bicyclo[3.2.1]octanes with one...
A Rh(III)-catalyzed intramolecular olefin hydroarylation of aromatic aldehydes with a transient directing group has been described. The bidentate groups in situ generated from and β-alanine could enable the subsequent C–H activation excellent site selectivities high functional compatibility. further conversion aldehyde showcased broad application prospects this methodology.
A Rh(III)-catalyzed undirected C–H activation/alkene insertion to synthesize diversified indole-fused polycyclics has been developed. Intramolecular electrophilic cyclization generated a 3-indolyl rhodium species that went through an aryl-to-aryl 1,4-rhodium migration realize the activation. The subsequent [4 + 2] carboannulation or hydroarylation of alkenes could be achieved, respectively, by simply adjusting additives reaction.
An unprecedented Pd-catalyzed alkyne insertion/C–H activation/intramolecular [4 + 2] carboannulation of alkenes has been reported. In this transformation, the C–H activation was triggered by an in situ generated alkenylpalladium species via cross-coupling reaction aryl iodides and alkynes. Subsequently, resulting five-membered C, C–palladacycle intermediates were added across alkenes, providing a unique approach to access diversified polycyclics good efficiency. Two new rings three C–C bonds...
Concomitant inhibition of MAPK and PI3K signaling pathways has been recognized as a promising strategy for cancer therapy, which effectively overcomes the drug resistance pathway-related inhibitors. Herein, we report scaffold-hopping generation series 1H-pyrazolo[3,4-d]pyrimidine dual ERK/PI3K Compound 32d was most candidate, with potent inhibitory activities against both ERK2 PI3Kα displays superior anti-proliferative profiles HCT116 HEC1B cells. Meanwhile, compound possessed acceptable...