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A chiral phosphoric acid‐catalyzed enantioselective aza‐Friedel–Crafts reaction of 5‐aminopyrazole derivatives with cyclic ketimines attached to a neutral functional group is reported. This protocol allows the formation of pyrazole‐based C2‐quaternary indolin‐3‐ones with high enantioselectivities and regioselectivities. Moreover, gram‐scale synthesis of the 5‐aminopyrazole‐based C2‐quaternary indolin‐3‐ones...
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