Search results for "DISCOVERY"

showing 10 items of 4119 documents

Tetramethylguanidine (TMG)-catalyzed addition of dialkyl phosphites to α,β-unsaturated carbonyl compounds, alkenenitriles, aldehydes, ketones and imi…

1998

Abstract Tetramethylguanidine-catalyzed addition of dialkyl phosphites to α,β-unsaturated carbonyl compounds, alkenenitriles, aldehydes and ketones constitutes a practical route to a variety of phosphonate synthons. The very mild conditions employed, together with the short reaction times, make the procedure highly versatile and tolerant to a range of functionalities. The proposed methodology is also convenient for the preparation of α-aminophosphonates.

chemistry.chemical_compoundChemistryOrganic ChemistryDrug DiscoverySynthonOrganic chemistryBiochemistryPhosphonateCatalysis
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Efficient preparation of 4-methoxy-5,6-dihydro-2H-pyran

2008

Abstract We report the efficient synthesis of 4-methoxy-5,6-dihydro-2 H -pyran (MDHP) via the TiCl 4 driven elimination of MeOH from 4,4-dimethoxytetrahydropyran. The previous difficulty of preparing MDHP restricted the wider use of 4-methoxytetrahydropyran-4-yl (MTHP) acyclic acetals, which have desirable protecting group properties when compared to more commonly used MOM- and THP-acetals. The behaviour of the elimination on related acetals is also examined.

chemistry.chemical_compoundChemistryPyranOrganic ChemistryDrug DiscoveryOrganic chemistryProtecting groupBiochemistryCombinatorial chemistryTetrahedron Letters
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Advances in singlet oxygen chemistry

2005

The authors discuss the advances made in both mechanistic and synthetic aspects of singlet oxygen chem.  Formation and reactions of singlet oxygen in heterogeneous media (such as zeolites, micelles, vesicles, etc.) are discussed.  Cycloaddns. of mol. oxygen to olefins, heteroatom oxidns. via reaction of singlet oxygen with the electron pair at heteroatoms, and photooxygenations of heterocyclic systems by singlet oxygen are also reviewed.

chemistry.chemical_compoundChemistrySinglet oxygenphotooxygenationOrganic ChemistryDrug Discoveryheteroatom oxidationPhotooxygenationGeneral MedicinePhotochemistryBiochemistrysinglet oxygenTetrahedron
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Antivirale Wirkstoffe, 17. Mitt. Oligocyclisch N-substituierte Lithocholsäureamide

1981

Von den durch Umsetzung der 3-Formyllithocholsaure mit den entsprechenden Aminen erhaltenen oligocyclisch N-substituierten Lithocholsaureamiden 1 uben insbesondere N-(2-Naphthyl)-3-formyllithocholsaureamid (1b) und N-(endo-2-Methylbicyclo[2.2.1]heptyl)lithocholsaureamid (1c) markante virustatische Wirkungen aus. Antiviral Drugs, XVII: Oligocyclically N-Substituted Lithocholic Amides Oligocyclically N-substituted lithocholic amides 1 are obtained by the reaction of 3-formyllithocholic acid with amines. N-(2-Naphthyl)-3-formyllithocholic amide (1b) and N-(endo-2-methylbicyclo-[2.2.1]heptyl)lithocholic amide (1c) exhibit marked virustatic activity.

chemistry.chemical_compoundChemistryStereochemistryAmideDrug DiscoveryPharmaceutical ScienceArchiv der Pharmazie
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Struktur-Wirkungs-Beziehungen bei Analeptica vom Typ des Nicethamids, 3. Mitt. Synthese von Analogen des 6-Methyl-nicethamids

1975

Als potentiell analeptisch wirksame Substanzen mit partiell fixierter funktioneller Gruppe werden strukturanaloge Amide, Imide und Lactame des 2-Methyl-nicethamids synthetisiert. Synthesis of 2-Methyl-Nicethamide Analogues. As potentially analeptically active substances with partially fixed functional groups, structural analogues of 2-methyl-nicethamide, in the form of amides, imides and lactams, are synthesized.

chemistry.chemical_compoundChemistryStereochemistryAmideDrug DiscoveryPharmaceutical ScienceStructure–activity relationshipImideArchiv der Pharmazie
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Verbindungen mit potentiell positiv inotroper Wirkung, 1. Mitt. N-Substituierte 3-Amino-2-cyclopentenone aus partiell hydrierten 2-Phenanthrylaminen

1984

Die Darstellung partiell hydrierter 2-Phenanthrylamine und ihre Umsetzung mit 1,3-Cyclopentandion zu N-subst. 3-Amino-2-cyclopentenonen wird beschrieben. Compounds with Potentially Positive Inotropic Activity, I: N-Substituted 3-Amino-2-cyclopentenones from Partially Hydrogenated 2-Phenanthrylamines The synthesis of partially hydrogenated 2-phenanthrylamines and their reactions with 1,3-cyclopentanedione to N-substituted 3-amino-2-cyclopentenones is described.

chemistry.chemical_compoundChemistryStereochemistryDrug DiscoveryPharmaceutical ScienceCondensation reactionEnoneEnamineArchiv der Pharmazie
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Massenspektrometrische Untersuchungen an Edukten für die Synthese H2-aktiver Substanzen

1982

Unter den Bedingungen der Elektronenstosionisation wurden 4-[(2-Aminoethoxy)-methyl]-5-methyl-imidazo (1), die Imidazolderivate mit N-substituierter Ethylendiamin-Struktur 2–5 sowie die Imidazolcarboxamide 6–8 massenspektrometrisch untersucht. Der Mechanismus der konkurrierenden Bindungsspaltungen und der Umlagerungsprozesse wird formuliert. Die Wechselwirkung der funktionellen Gruppen sowie deren Einflus auf das Fragmentationsverhalten der Substanzen wird beschrieben und ein Schema der Hauptfragmentierungswege vorgeschlagen. Mess Spectrometry of Reactants for the Synthesis of H2-Active Compounds 4-[(2-Aminoethoxy)methyl]-5-methylimidazole (l), the imidazoles 2-5 with N-substituted ethylene…

chemistry.chemical_compoundChemistryStereochemistryDrug DiscoveryPharmaceutical ScienceImidazolcarboxamideElectron impact mass spectrometryEthylenediamineArchiv der Pharmazie
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Histaminähnliche Verbindungen mit cyclisierter Seitenkette 1. Mitt. über Struktur-Wirkungs-Beziehungen bei Histaminanaloga

1973

Als potentiell histaminartig wirksame Substanzen wurden 4-substituierte Piperidyl- und Aminocyclohexyl-imidazole dargestellt. Von diesen erwiesen sich 4-(3-Piperidyl)-imidazol (4b) und 4-(2-Aminocyclohexyl)-imidazol (8a) als histaminomimetisch wirksam. Uber Struktur-Wirkungs-Beziehungen der Histaminanaloga mit cyclisierter Seitenkette des Histaminmolekuls wird be richtet. Histamine-like Compounds with Cyclized Side Chain As substances with possible histamine-like activity 4-substituted piperidyl- and aminocyclohexyl-imidazoles were prepared. Two of them, 4-(3-piperidyl)-imidazole (4b) and 4-(2-aminocyclohexyl)-imidazole (8a), have histamine-like activity. Structure-action relationships of h…

chemistry.chemical_compoundChemistryStereochemistryDrug DiscoverySide chainPharmaceutical ScienceHistamineArchiv der Pharmazie
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A DFT study for the formation of imidazo[1,2-c]pyrimidines through an intramolecular Michael addition

2006

The formation of imidazo[1,2-c]pyrimidines through a ring closure of 2-(2-sulfonylimino-1,2-dihydro-1-pyrimidinyl) acetamides has been studied using DFT methods. Analysis of the energy results for the cyclization step shows the demand of almost an acid catalyst, which increases the electrophilicity of the dihydropyrimidine moiety, in order to make feasible the intramolecular Michael addition. The substitution on both dihydropyrimidine and amide moieties has also an influence on the cyclization step.

chemistry.chemical_compoundChemistryStereochemistryIntramolecular forceAmideOrganic ChemistryDrug DiscoveryElectrophileMichael reactionMoietyRing (chemistry)BiochemistryCatalysisTetrahedron
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Bonandiol: A new, irregular, monocyclic diterpene from (L.) Halacsy (umbelliferae)

1984

A new, irregular, monocyclic diterpene, bonandiol (1), has been isolated from Bonannia graeca. The structure of bonandiol has been deduced from spectral data and chemical evidence.

chemistry.chemical_compoundChemistryStereochemistryOrganic ChemistryDrug DiscoveryMoleculeDiterpeneSpectral dataBiochemistryTetrahedron Letters
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