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Review reveals progress in asymmetric synthesis of C2 chiral indolin-3-ones, suggesting new methodologies for chiral drug development.
Compounds containing 2,2-disubstituted indoline-3-one skeletons are widely used in many fields such as natural products and chiral drugs.The efficient construction of 2,2-disubstituted indolin-3-ones by asymmetric catalysis has attracted more and more attention.The research progress in the asymmetric synthesis of 2,2-disubstituted indolin-3-ones using 2-substituted indolin-3-ones as substrates in recent years is reviewed, including asymmetric aza-Friedel-Crafts reaction, Mannich reaction, aza-Diels-Alder reaction, aza-Henry reaction, aza-Morita-Baylis-Hillman reaction and other reactions.It provides a reference for the future asymmetric synthesis of C2 quaternary carbon center indolin-3-one compounds.Keywords 2-aryl-3H-indol-3-ones; asymmetric catalysis; C2-quaternary indolin-3-ones C2 -3- [1] , Isatisine A Isatisine A acetonide ( 1)-1 (HIV-1) C8166 T [2] . C2 -3- , Mitragynine pseudoindoxyl Mitragynine , 7-Hydroxymitragynine , mitragynine 7-HMG , , [3] .
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Qiao et al. (2025) studied this question.
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