Abstract

AbstractDiastereoisomeric pyrazolone‐fused spirocyclohexenimines, bearing contiguous all‐carbon quaternary and tertiary stereocenters, are readily synthesized for the first time in good to excellent yield (up to 98%) and high enantioselectivity (up to 97% ee) via vinylogous Michael reaction/cyclization cascade reaction of α‐arylidene pyrazolones and α,α‐dicyanoalkylidenes. The formal [4+2] atom‐economical annulation proceeds with commercially available Takemoto's catalyst under mild reaction conditions. Scale‐up reaction and post‐transformation of the products were also demonstrated.magnified image

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