Search results for "Electrophile"

showing 10 items of 258 documents

First Electrophilic Substitutions of 3-Substituted Indoles with Diethoxycarbenium Tetrafluoroborate: Functionalized Indole Derivatives

1990

The indoles 2a-2c react with diethoxycarbenium tetrafluoroborate (1) to furnish the indolecarbaldehydes 3a-3d. In the thermodynamically controlled reaction of 3-methylindole (2a) with 1 the tris(indolyl)methane 4 and diskatole (5), are formed in addition. The limitations of these reactions are discussed and evidence is presented for a C-3-ipso-attack and a Wagner-Meerwein rearrangement, respectively, leading to the formation of 3b or 3d. Erste elektrophile Substitution von 3-substituierten Indolen mit Diethoxycarbenium-Tetrafluoroborat: Funktionalisierte Indol-Derivate Die Indole 2a-2c reagieren mit dem per se synthetisierten Diethoxycarbenium-Tetrafluoroborat (1) zu den Indolcarbaldehyden …

chemistry.chemical_classificationIndole testWagner–Meerwein rearrangementTetrafluoroborateBicyclic moleculeChemistrymedicine.drug_classStereochemistryPharmaceutical ScienceCarboxamideAldehydechemistry.chemical_compoundElectrophilic substitutionDrug DiscoveryElectrophilemedicineArchiv der Pharmazie
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Understanding the regio- and chemoselective polar [3+2] cycloaddition of the Padwa carbonyl ylides with α-methylene ketones. A DFT study

2009

The regio- and chemoselective polar [3+2] cycloaddition (32CA) of the Padwa carbonyl ylide (CY) with α-methylene ketone (αMK) to yield the oxa-bridged spirocycloadduct has been studied using the DFT method at the B3LYP/6-31G(d) computational level. Six reactive channels associated to the stereo-, regio-, and chemoselective approach modes of the CY to the CC and CO reactive sites of the αMK have been analyzed. DFT calculations for this cycloaddition are in complete agreement with the experimental outcome, explaining the reactivity and selectivity of the formation of the [3+2] cycloadduct. Analysis of the global and local electrophilicity and nucleophilicity indices allows an explanation abou…

chemistry.chemical_classificationKetoneStereochemistryOrganic ChemistryRegioselectivityBiochemistryCycloadditionReaction coordinatechemistryNucleophileYlideComputational chemistryDrug DiscoveryElectrophileChemoselectivityTetrahedron
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First reactions of dialkoxycarbenium tetrafluoroborates with pyrroles, 5H-dibenz[b,f]azepines, and electron-rich arenes

2009

Pyrrole (2a) and 2,5-dimethylpyrrole (2b) react with the dialkoxycarbenium tetrafluoroborates 1a-1c under kinetic control to yield the corresponding acylpyrrole derivatives. 5H-Dibenz[b,f]azepine (9a) and the 10,11-dihydro derivative 9b react only with the most electrophilic of the series of electrophiles tested, namely, diethoxycarbenium tetrafluoroborate (1a), to furnish the corresponding formyl derivatives. Similarly, in arene chemistry, the highly electron-rich N,N-dimethylaniline (13a) and 1,3,5-trimethoxybenzene (13b) are formylated by reaction with 1a.

chemistry.chemical_classificationKetoneTetrafluoroborateTertiary amineOrganic ChemistryRegioselectivityMedicinal chemistryFormylationchemistry.chemical_compoundchemistryElectrophileOrganic chemistryAzepinePyrroleJournal of Heterocyclic Chemistry
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Five-to-Six Membered Ring-rearrangements in the Reaction of 5-Perfluoroalkyl-1,2,4-oxadiazoles with Hydrazine and Methylhydrazine

2006

The hydrazinolysis reaction of 5-perfluoroalkyl-1,2,4-oxadiazoles with hydrazine or methylhydrazine as bidentate nucleophiles has been investigated. The reaction occurred through the addition of the bidentate nucleophile to the C(5)-N(4) double bond of the 1,2,4-oxadiazole followed by ring-opening and ring-closure (ANRORC) involving the second nucleophilic site of the reagent. This ring-closure step could involve either the original C(3) of the 1,2,4-oxadiazole (giving a five-to-five membered ring rearrangement) or an additional electrophilic center linked to it (exploiting a five-to-six membered ring rearrangement). An alternative initial nucleophilic attack may involve the additional elec…

chemistry.chemical_classificationMethylhydrazineKetoneDouble bondChemistryStereochemistryTRANSFORMATIONS15N-NMR SPECTROSCOPYCHEMICAL SHIFT CALCULATIONSOrganic ChemistryFLUORINATED HETEROCYCLIC-COMPOUNDSHydrazoneRegioselectivityBKR REARRANGEMENTRing (chemistry)EXPEDIENT ROUTEMOLECULAR-REARRANGEMENTSNucleophileAROMATICITY INDEXElectrophileATTACKFIVE TO SIX REAGGANGEMENT
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Quantitative characterization of the global electrophilicity pattern of some reagents involved in 1,3-dipolar cycloaddition reactions

2003

Abstract The global electrophilicity power, ω, of a series of dipoles and dipolarophiles commonly used in 1,3-dipolar cycloadditions may be conveniently classified within a unique relative scale. The effects of chemical substitution on the electrophilicity of molecules have been evaluated using a representative set of electron-withdrawing and electron-releasing groups for a series of dipoles including nitrone, nitrile oxide and azide derivatives. The absolute scale of electrophilicity is used to rationalize the chemical reactivity of these species as compared to the static reactivity pattern of the reagents involved in the Diels–Alder reactions.

chemistry.chemical_classificationNitrileOrganic ChemistryPhotochemistryBiochemistryNitronechemistry.chemical_compoundchemistryComputational chemistryReagentDrug DiscoveryElectrophile13-Dipolar cycloadditionMoleculeReactivity (chemistry)AzideTetrahedron
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Understanding the origin of the asynchronicity in bond-formation in polar cycloaddition reactions. A DFT study of the 1,3-dipolar cycloaddition react…

2012

The origin of the asynchronicity in bond-formation in polar cycloadditions has been studied by an ELF analysis of the electron reorganisation along the 1,3-dipolar cycloaddition of Padwa's carbonyl ylide 4 with the 1,2-benzoquinone 8. This reaction presents an unexpected asynchronous bond-formation, which is initialised through the nucleophilic attack of Padwa's carbonyl ylide on the carbonyl oxygen atom of the strongly electrophilically activated 1,2-benzoquinone. The present study allows for the establishment that along an asynchronous bond-formation, the more favourable two-center interaction begins at the most electrophilic center, which is the center with the highest spin density achie…

chemistry.chemical_classificationNucleophileChemistryYlideGeneral Chemical EngineeringElectrophile13-Dipolar cycloadditionPolarGeneral ChemistrySpin densityBond formationPhotochemistryCycloadditionRSC Adv.
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Reactivity of the carbon-carbon double bond towards nucleophilic additions. A dft analysis

2004

Abstract The global and local electrophilicity indexes have been used to characterize the reactivity pattern of the CC double bond towards nucleophilic addition reactions. A wide family of molecules including ketones, esters, anhydrides, nitriles and nitrocompounds containing appropriate substitution on the CC double bond have been classified within an unique scale of reactivity. The predictive capability of the theoretical model is tested against a series of benzylidenemalononitriles and substituted α-nitrostilbenes.

chemistry.chemical_classificationNucleophilic additionDouble bondOrganic ChemistryReinforced carbon–carbonBiochemistrychemistryNucleophileComputational chemistryDrug DiscoveryElectrophileOrganic chemistryMoleculeDensity functional theoryReactivity (chemistry)
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Reactivity of the di-μ-hydroxo-complexes [{Pd(NN)}2(μ-OH)2][ClO4]2 (NN=bis(pyrazol-1-yl)alkanes) towards protic electrophiles. Hydration of coordin…

2000

Abstract The hydroxo-complexes [{Pd(μ-OH)(NN)}2][ClO4]2 (NN=bpzm:bis(pyrazol-1-yl) methane: a-compounds, bpzm*:bis(3,5-dimethylpyrazol-1-yl)methane; b-compounds) react with a wide variety of weak protic electrophiles H(LL) in a 1:2 molar ratio to give the mononuclear cationic palladium(II) derivatives of general formula [Pd(LL)(NN)][ClO4] [LL=2-pyridine-methoxo (OCH2-py) (1a,b); picolinate (pic) (2a,b); 8-hydroxiquinolinate (oxin) (3a,b)] or the dinuclear complexes [{Pd(NN)}2(μ-ox)][ClO4]2 [ox=oxalate: (4a,b)] and [{Pd(μ-LL)(NN)}2][ClO4]2 [LL=pyrazolate (pz) (5a,b); p-thiocresolate (SC6H4Me-p) (6a,b); triazolate (tz) (7b); thiophenolate (SPh) (8b)] when reacting with oxalic acid, azole…

chemistry.chemical_classificationNucleophilic additionStereochemistrychemistry.chemical_elementCrystal structureMedicinal chemistryOxalateInorganic Chemistrychemistry.chemical_compoundDeprotonationchemistryElectrophileMaterials ChemistryReactivity (chemistry)Physical and Theoretical ChemistryDithiocarbamatePalladiumPolyhedron
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A DFT study of the Huisgen 1,3-dipolar cycloaddition between hindered thiocarbonyl ylides and tetracyanoethylene

2004

Abstract The mechanism for the 1,3-dipolar cycloaddition between the hindered thiocarbonyl ylide 1 and tetracyanoethylene 2 has been studied at the B3LYP/6-31G ∗ level. Formation of the [3+2] cycloadduct 4 takes place through a stepwise mechanism that is initiated by the nucleophilic attack of the thiocarbonyl ylide 1 to the ethylene derivative 2 to give a zwitterionic intermediate IN . The subsequent cyclization of IN yields a seven-membered cyclic ketene imine 6 , which equilibrates with the thermodynamically more stable [3+2] cycloadduct 4 . The computed free energies are in agreement with the experimental outcomes.

chemistry.chemical_classificationOrganic ChemistryImineKeteneTetracyanoethylenePhotochemistryBiochemistryMedicinal chemistryCycloadditionchemistry.chemical_compoundchemistryNucleophileYlideDrug DiscoveryElectrophile13-Dipolar cycloadditionTetrahedron
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Alkylation of lithium dienediolates of butenoic acids. Regioselectivity effects of structure and leaving group of the alkylating agent

1998

Abstract Regioselectivity of alkylation of but-2-enoic acids 1 and 2 by alkyl halides strongly depends on the reactivity of the electrophile. High α selectivity results for saturated alkyl halides, whereas poor α-selectivity is obtained for highly reactive allyl and benzyl halides. For reactive alkylating halides selectivity is partly governed by the ion pairing aggregates of the dienediolates. Lithium bromide and the carboxylate generated in the ongoing reaction cause opposite effects on regioselectivity.

chemistry.chemical_classificationOrganic ChemistryLeaving groupRegioselectivityAlkylationBiochemistryMedicinal chemistrychemistry.chemical_compoundchemistryDrug DiscoveryElectrophileOrganic chemistrylipids (amino acids peptides and proteins)Reactivity (chemistry)CarboxylateSelectivityAlkylTetrahedron
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