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摘要
A one-pot catalytic asymmetric route to novel chiral quaternary-carbon-containing cyclobutanone-fused 4-aminoquino-line derivatives in good to high yields and enantioselectivities is described. This process consists of a chiral phosphoric acid -catalyzed desymmetric carbonyl-amine condensation of prochiral cyclobutane-1,3-diones with 2-halogenated anilines and a Pd -catalyzed coupling reaction of the chiral enaminone intermediates with isocyanides. R1 NHt-Bu O N "R Me 22 examples 40-93%, up to 97% ee Pd(0) 1 t-BuNC
