Enantioselective C-H Arylation: New Menthod For Synthesis Of P-chiral Compounds

In this thesis, a novel and facile method for the synthesis ofhighly enantioenriched P-chiral compounds throughpalladium-catalyzed intramolecular enantioselective C-H activationwas developed. The substrates were prepared fromdiarylphosphinyl chloride as the initial material, by their aminationwith2-bromo-anilines and the subsequent alkylation steps. Afterestablishing the initial template reaction, we further investigateddifferent factor for the reaction which include chiral phosphineligands, reaction temperature, additives, proportion of palladium,palladium source, base and solvent in the reaction, and found thattaddol-based phosphoramidite ligands showed the highestenantioselectivity towards the reaction. After determining theoptimal reaction conditions, then we expanded the substr ates. Theexperimental results showed that a variety of phosphoramides withdifferent substituents were well tolerated in the reaction, and to99%yield and up to97%ee was achieved.