Search results for "DISCOVERY"

showing 10 items of 4119 documents

A comparative study of the multicomponent Ugi reactions of an oxabicycloheptene-based β-amino acid in water and in methanol

2006

Di-exo-3-amino-7-oxabicyclo[2.2.1]hept-5-ene-2-carboxylic acid 1, five aldehydes and two isocyanides were reacted both in methanol and in water to prepare a 10-membered β-lactam library via a Ugi-4-centre-3-component reaction. The yields were found to be similar in water and methanol. The diastereoselectivities of the aqueous reactions were similar, though in a few cases higher than those in methanol. The benefits of water are the facile isolation of the precipitated product and the shorter reaction time.

chemistry.chemical_classificationchemistry.chemical_compoundAqueous solutionChemistryOrganic ChemistryDrug DiscoveryOrganic chemistryMethanolBiochemistryAmino acidTetrahedron Letters
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Synthetic methods for the preparation of polystyrene resins containing chiral polyamine chains

1998

Abstract The preparation of functionalized polystyrene-divinylbenzene resins containing functional groups derived from polyamine aliphatic chains has been studied. Best results are always obtained by direct alkylation of the polyamine with Merrifield's polymers, but double alkylation at both end of the polyamine is observed. The procedure is useful for the preparation of polymer containing different chiral and non-chiral polyamine functionalities.

chemistry.chemical_classificationchemistry.chemical_compoundChemistryOrganic ChemistryDrug DiscoveryPolymer chemistrytechnology industry and agricultureOrganic chemistryPolymerPolystyreneAlkylationPolyamineBiochemistryTetrahedron
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Polyenolates of unsaturated carboxylic acids in synthesis. A straightforward synthesis of retinoic acids.

1990

Abstract Retinoic acids are prepared in a two step procedure by addition of lithium trienediolates of sorbic acid and 3-methyl-sorbic acid to β-ionone.

chemistry.chemical_classificationchemistry.chemical_compoundChemistryOrganic ChemistryDrug DiscoveryTwo stepFatty acidchemistry.chemical_elementOrganic chemistryLithiumSorbic acidBiochemistryTetrahedron Letters
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Mukaiyama-type, eight-membered ring closure: Access to a tricyclic system related to taxanes

1998

Abstract Addition of Me2CuLi, with in situ trapping by TMSCl, to Hagemann's ester derivative 13, furnished silyl enol ether 14. Mukaiyama-type cyclization of the latter compound gave the tricyclic derivative 15, structurally related to the taxane core.

chemistry.chemical_classificationchemistry.chemical_compoundChemistryStereochemistryOrganic ChemistryDrug DiscoverySilyl enol etherRing (chemistry)BiochemistryDerivative (chemistry)TricyclicTetrahedron Letters
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- conformational preference of , -9-oxobicyclo[3.3.1]nonane-2,4-dicarboxylic acid

1985

Abstract The 1 H and 13 C nmr spectra of exo , exo -9-oxobicyclo[3.3.1]nonane-2,4-dicarboxylic acid, 3, in DMSO-d 6 or alkaline D 2 O, clearly show that it exists in a boat - chair -conformation with equatorial carboxyl groups, thus being the first case of boat - chair preference of a bicyclo[3.3.1] nonan-9-one due to the presence of exo , exo -2,4- substituents.

chemistry.chemical_classificationchemistry.chemical_compoundDicarboxylic acidchemistryBicyclic moleculeStereochemistryOrganic ChemistryDrug DiscoveryNuclear magnetic resonance spectroscopyCarbon-13 NMRNonaneBiochemistryTetrahedron Letters
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Imidazolsynthesen, Mitt. Synthese α-substituierter 4(5)-Methoxymethyl-5(4)-methyl-imidazole

1977

Methoxymercurierung der α,β-ungesattigten Ketone 1 ergibt α-Acetoxymercuri-β-methoxy-ketone 2, die direkt zu α-Brom-β-methoxy-ketonen 3 bromo- demercuriert werden. Cyclisierung von 3 mit Formamidinacetat in flussigem Ammoniak fuhrt zu α-substituierten 4(5)-Methoxy-methyl-5(4)-methyl-imidazolen 4, deren Struktur 13C-NMR-spektroskopisch gesichert ist. Synthesis of α-Substituted 4(5)-Methoxymethyl-5(4)-methylimidazoles Methoxymercuration of the α,β-unsaturated ketones 1 produces the α-acetoxymercury-β-methoxyketones 2, which are bromo-demercurised without isolation to give the α-bromo-β-methoxyketones 3. Cyclisation of 3 with formamidine acetate in liquid ammonia leads to α-substituted 4(5)-me…

chemistry.chemical_classificationchemistry.chemical_compoundKetoneFormamidine acetatechemistryStereochemistryDrug DiscoveryLiquid ammoniaPharmaceutical ScienceImidazoleMedicinal chemistryArchiv der Pharmazie
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Enantioselective synthesis of sabina ketone

2003

Both enantiomers of sabina ketone were efficiently prepared via an easy synthesis of 1-diazo-5-methylene-6-methylheptan-2-one, starting from succinic anhydride, followed by its highly enantioselective cyclization catalyzed by chiral dirhodium(II) compounds having ortho-metalated phosphines as ligands.

chemistry.chemical_classificationchemistry.chemical_compoundKetonechemistryOrganic ChemistryDrug DiscoverySuccinic anhydrideEnantioselective synthesisOrganic chemistryEnantiomerBiochemistryCatalysisTetrahedron Letters
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Separation of amino acid enantiomers using supported liquid membrane extraction with chiral phosphates and phosphonates

1999

A series of dialkyl and monoalkyl phosphates, phosphites and phosphinates based on (−)-menthol and (−)-nopol were synthesized and used as carriers for transport of aromatic amino acids through supported liquid membranes. Although all the compounds were found to be effective carriers (with transport rate dependent on their structure) the enantioselectivity of the process obtained was low or moderate. Aromatic amino acids were enantioselectively transported through supported liquid membranes containing chiral phosphates, phosphites and phosphinates as carriers. Download full-size image

chemistry.chemical_classificationchemistry.chemical_compoundMembranechemistryOrganic ChemistryDrug DiscoveryExtraction (chemistry)Rate dependentAromatic amino acidsOrganic chemistryEnantiomerBiochemistryAmino acidTetrahedron
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Efficient synthesis of novel pyrido[3,2-d]pyrimidine-2,4-diones

2003

Abstract A series of pyrido[3,2- d ]pyrimidine-2,4-diones 5a – g have been synthesized through conversion of 2,3-pyridinedicarboxylic anhydride 1 into half-ester 2 , subsequent Curtius rearrangement and further reaction with amino acids.

chemistry.chemical_classificationchemistry.chemical_compoundPyrimidinechemistryStereochemistryOrganic ChemistryDrug DiscoveryOrganic chemistryGeneral MedicineBiochemistryCurtius rearrangementAmino acidTetrahedron Letters
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Mechanismus und Reaktionswege der Xanthenylierung an ambidenten nukleophilen Arzneistoffen

1986

Am Beispiel der ambidenten nukleophilen Arzneistoffe 4-Aminobenzolsulfonamid (3), Indometacin (7) und Phenylbutazon (10) werden Aralkylierungen mit dem SN1-aktiven Reagens Xanthydrol (1) vorgestellt. Mechanism and Reaction Path of the Xanthenylation of Ambident Nucleophilic Drugs The aralkylation of ambident nucleophilic drugs, e.g. 4-aminobenzenesulfonamide (3), indometacine (7) and phenylbutazone (10), with SN1-active xanthydrol (1) is described.

chemistry.chemical_classificationchemistry.chemical_compoundSN1 reactionNucleophileBicyclic moleculechemistryStereochemistryDrug DiscoveryPharmaceutical ScienceReaction pathXanthydrolSulfonamideArchiv der Pharmazie
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