Search results for "2-oxindole"

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Regio- and Stereoselective Synthesis of 3-Pyrazolylidene-2-oxindole Compounds by Nucleophilic Vinylic Substitution of (E)-3-(Nitromethylene)indolin-2…

2019

[EN] A highly regio- and stereoselective synthesis of 3-alkylidene-2-oxindoles has been described through a nucleophilic vinylic substitution (SNV) of (E)-3-(nitromethylene)indolin-2-one using pyrazol-3-ones as nucleophiles and Et3N as a base. The reaction affords selectively the Z-isomer when pyrazol-3-ones without substituents at the 4 position are used. While the reaction is E-selective with 4- substituted pyrazolones. The stereoselectivity (up to >20:1) and the yields (up to 98%) are very high under mild reaction conditions.

010405 organic chemistryChemistryStereochemistryEstereoquímica2-oxindoleSubstitution (logic)2-oxindoleStereoselectivityGeneral ChemistryIndolin 2 one010402 general chemistry01 natural sciences0104 chemical sciencesReaccions químiquesRegioselectivityNucleophileFISICA APLICADAmedia_common.cataloged_instancePyrazoloneStereoselectivityEuropean unionmedia_commonVinylic substitution
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Direct synthesis of C3-mono-functionalized oxindoles from N-unprotected 2-oxindole and their antileishmanial activity.

2014

A novel approach for the synthesis of unprecedented C3-mono-functionalized indolin-2-ones is reported, starting from 2-oxindole and chalcones. The reactions proceed regioselectively under mild conditions, without di- and tri-alkylated side products. The new compounds have been evaluated in vitro for their antiproliferative effects against the protozoan Leishmania infantum. Interestingly, they appear able to kill L. infantum promastigotes and amastigotes, without significant cytotoxic effects.

DiastereoselectivityLeishmanicidal activityIndolesStereochemistryClinical BiochemistryAntiprotozoal AgentsDrug Evaluation PreclinicalPharmaceutical Science2-oxindoleChemistry Techniques SyntheticBiochemistryCell LineMiceStructure-Activity RelationshipChalconeMichael additionparasitic diseasesDrug DiscoveryToxicity TestsAnimalsLeishmania infantumAmastigoteMolecular BiologyLeishmaniaOxindoles; Michael addition; Leishmania; Leishmanicidal activity; Diastereoselectivity; CyclizationbiologyDose-Response Relationship DrugChemistryOrganic Chemistrybiology.organism_classificationLeishmaniaCombinatorial chemistryIn vitroOxindolesCyclizationMichael reactionMolecular MedicineOxindoleLeishmania infantumBioorganicmedicinal chemistry
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