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showing 10 items of 8115 documents

ChemInform Abstract: Indirect Regioselective Heteroarylation of Indoles Through a Friedel-Crafts Reaction with (E)-1,4-Diaryl-2-buten-1,4-diones.

2010

Abstract A two-step synthesis of 3-heteroaryl indoles has been developed. The first step of the sequence involves a Friedel–Crafts alkylation of indoles with 1,4-diaryl-2-buten-1,4-diones to give the corresponding indoles bearing a 1,4-dicarbonyl moiety. The reaction is catalyzed by InCl 3 and takes place with good yields. Cyclization of the diones under different Paal–Knorr conditions allows to prepare indoles substituted at the C3 position with 3-furanyl, 3-pyrrolyl- and 3-thienyl moieties.

ChemistryMoietyRegioselectivityGeneral MedicineAlkylationThiophene derivativesMedicinal chemistryFriedel–Crafts reactionPyrrole derivativesCatalysisChemInform
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Solution Processed Micro- and Nano-Bioarrays for Multiplexed Biosensing

2012

This Feature article reports on solution dispensing methodologies which enable the realization of multiplexed arrays at the micro- and nanoscale for relevant biosensing applications such as drug screening or cellular chips.

ChemistryNanotechnologyBiosensing TechniquesElectrochemical TechniquesEquipment DesignHardware_PERFORMANCEANDRELIABILITYMicroarray AnalysisMultiplexingHigh-Throughput Screening AssaysAnalytical ChemistrySolution processedNano-Hardware_INTEGRATEDCIRCUITSAnimalsHumansNanotechnologyBiochipBiosensorAnalytical Chemistry
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Indirect regioselective heteroarylation of indoles through a Friedel–Crafts reaction with (E)-1,4-diaryl-2-buten-1,4-diones

2009

Abstract A two-step synthesis of 3-heteroaryl indoles has been developed. The first step of the sequence involves a Friedel–Crafts alkylation of indoles with 1,4-diaryl-2-buten-1,4-diones to give the corresponding indoles bearing a 1,4-dicarbonyl moiety. The reaction is catalyzed by InCl 3 and takes place with good yields. Cyclization of the diones under different Paal–Knorr conditions allows to prepare indoles substituted at the C3 position with 3-furanyl, 3-pyrrolyl- and 3-thienyl moieties.

ChemistryOrganic ChemistryDrug DiscoveryRegioselectivityOrganic chemistryMoietyAlkylationBiochemistryFriedel–Crafts reactionCatalysisTetrahedron
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A DFT study of the mechanism of Brønsted acid catalysed Povarov reactions

2015

Abstract The molecular mechanism of the Bronsted acid (BA) catalysed Povarov reaction of N -phenyl- C -methoxycarbonyl imine with a methylenecyclopropane (MCP) has been investigated using DFT methods at the MPWB1K/6-31G(d) level. This BA catalysed Povarov reaction is a domino process initialised by the formation of a cationic intermediate which experiences a quick intramolecular Friedel–Crafts reaction yielding the final tetrahydroquinoline. Protonation of the imine nitrogen atom notably increases the electrophilicity of the corresponding species, accelerating the reaction through ionic processes. Analysis of the Parr functions in the initial nucleophilic attack of MCP to the protonated imi…

ChemistryOrganic ChemistryImineRegioselectivityProtonationPhotochemistryMethylenecyclopropaneBiochemistryMedicinal chemistrychemistry.chemical_compoundNucleophileDrug DiscoveryElectrophilePovarov reactionBrønsted–Lowry acid–base theoryTetrahedron
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Addition of dianions of carboxylic acids to imines. Influence of the acid in the outcome of the reaction

2009

Gil Grau, Salvador, Salvador.Gil@uv.es, Parra Alvarez, Margarita, Margarita.Parra@uv.es, Rodriguez Abad, Pablo, roapa@alumni.uv.es

ChemistryOrganic ChemistryRegioselectivityOrganic chemistryArkivoc
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Reactivity and Selectivity of Ortho-Metalated Rhodium(II) Complexes in C−H Insertion Reactions of α-Diazo Compounds

1998

Regioselective intramolecular C−H insertion reactions of α-diazo β-keto esters and α-diazo ketones are mediated by Rh2[OOCR]4-x[PC]x (x = 1, 2; PC = ortho-metalated phosphine; R = CH3, C3F7). In particular, the intramolecular transformation of 1-diazo-5-methyl-3-propyl-2-hexanone catalyzed by Rh2[OOCCH3]2[PC]2 (PC = (C6H4)P(C6H5)2, head-to-tail (H−T) configuration) afforded only the tertiary C−H insertion product. By comparison, no C−H insertion reaction was promoted by doubly metalated complexes with a head-to-head (H−H) configuration. Rh2[OOCR]3[PC] compounds were found to be less suited for these type of reactions.

ChemistryOrganic ChemistryRegioselectivitychemistry.chemical_elementMedicinal chemistryRhodiumInorganic Chemistrychemistry.chemical_compoundInsertion reactionIntramolecular forceDiazoReactivity (chemistry)Physical and Theoretical ChemistrySelectivityPhosphineOrganometallics
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Gold(I)-Catalyzed Reactions of 1-(ortho-Alkynylaryl)ureas: Highly Selective Heterocyclization and Synthesis of MixedN,O-Acetals

2014

Treatment of alkynylureas (I) with trifluoroethanol in the presence of a Au/Ag catalytic system provides N-6-exo-dig heterocyclization products (III) and in some cases open chain acetals as side products.

ChemistryOrganic chemistryRegioselectivityGeneral ChemistryHydroaminationHighly selectiveCatalysisAdvanced Synthesis & Catalysis
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ChemInform Abstract: Enantioselective Mannich Reaction of β-Keto Esters with Aromatic and Aliphatic Imines Using a Cooperatively Assisted Bifunctiona…

2015

The title reaction tolerates aliphatic and aromatic substituents on both reaction partners, affording products (III) as a mixture of inseparable diastereomers with low or without any diastereoselectivity.

ChemistryOrganocatalysisEnantioselective synthesisDiastereomerOrganic chemistryGeneral MedicineMannich reactionBifunctional catalystChemInform
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Organocatalytic asymmetric addition of naphthols and electron-rich phenols to isatin-derived ketimines: highly enantioselective construction of tetra…

2015

A quinine-derived thiourea organocatalyst promoted the highly enantioselective addition of naphthols and activated phenols to ketimines derived from isatins. The reaction afforded chiral 3-amino-2-oxindoles with a quaternary stereocenter in high yields (up to 99%) with excellent enantioselectivity (up to 99% ee). To the best of our knowledge, this transformation is the first highly enantioselective addition of naphthols to ketimines

ChemistryOrganocatalysisIsatinIsatin-derived ketiminesEnantioselective synthesisAsymmetric synthesisGeneral ChemistryNaphtholsGeneral MedicineCatalysisStereocenterReaccions químiqueschemistry.chemical_compoundThioureaCatàlisiOrganocatalysisFISICA APLICADAOrganic chemistryPhenolsFriedel-Crafts reactionsQuímica orgànicaAngewandte Chemie (International ed. in English)
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Asymmetric Synthesis of Dihydropyranones with Three Contiguous Stereocenters by an NHC‐Catalyzed Kinetic Resolution

2021

An oxidative NHC-catalyzed kinetic resolution (KR) of racemic mixtures is presented. The developed reaction furnishes tricyclic dihydropyranones with three contiguous stereocenters in excellent dia- and enantioselectivity, with good-to-moderate yields. Mechanistic studies indicate that the rate-determining step of the reaction is the formation of the Breslow intermediate, while the selectivity determining step occurs later in the mechanism. The presented methodology enables rapid synthesis of complex structures in a single step.

ChemistryOrganocatalysisOrganic ChemistryEnantioselective synthesisSingle stepPhysical and Theoretical ChemistrySelectivityCombinatorial chemistryCatalysisKinetic resolutionStereocenterEuropean Journal of Organic Chemistry
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