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Showing 1 to 20 of 22 for “"carboxamides"”.
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Direction and Stabilization of Alpha' and Beta Metalations by Tertiary Carboxamides
Metalations $\alpha\sp\prime$ and $\beta$ to a tertiary amide have been investigated. Control and understanding of the regiochemistry of these novel metalations is discussed.
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Design, synthesis and biological evaluation of novel tetra-substituted quinoline-3-carboxamides derivatives
… synthesis of novel tetra-substituted quinoline-3carboxamides and subsequent transformation to other novel derivatives and evaluation of their biological activities against malaria and cytotoxicity. In achieving the objective, 2-chloroquinoline-3-carbaldehyde analogues 54A-G were synthesised from …
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Remote Lithiations of Carboxamides: The Manifestation of a Post-Complexation Proximity Effect (Homoenolate)
The remote metalations of tertiary amides, (beta) and (gamma) substituted with vinyl, phenyl and thiophenol groups, are reported. N,N-Diisopropyl-2-methylpent-4-enecarboxamide (59), N,N-diisopropyl-2-methyl-3-phenylpropanecarboxamide (139), N,N-diisopropyl-2-methyl-3-phenylthiopropanecarboxamide …
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Beta-lithiations of carboxamides: An investigation of the regio- and stereoselectivity of directed lithiations
An investigation of the diastereoselective $\beta$-metalation and of the structure of a carbanion of a $\beta$-phenyl tertiary amide has been carried out. The directed metalation has been found to occur with high diastereoselectivity and the resulting carbanion is best described as a pyramidal …
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Small Core Heterocyclic Carbamates and Carboxamides: Resistance-breaking Acetylcholinesterase Inhibitors Targeting the Malaria Mosquito, Anopheles gambiae
… diffraction. Several of the novel carbamates and carboxamides evaluated exhibited excellent toxicity towards susceptible G3 and resistant Akron strain An. gambiae (48f LC₅₀ G3 = 41 μg/mL, LC₅₀ Akron = 58 μg/mL, and 47i LC₅₀ G3 = 38 μg/mL, LC₅₀ Akron = 40 μg/mL). Hence, achieving the resistance- …
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Ring-Opening of Aziridine -2 -Carboxamides by Carbohydrate C1-O Nucleophiles. Stereoselective Preparation of O-Linked Glycopeptides
… C1-O nucleophilic ring-opening of aziridine-2-carboxamides to access the target O-linked glycopeptides. The synthesis of the alpha-GalNAc-Ser class of glycopeptides is emphasized and either the alpha- or beta-glycoside can be accessed by judicious selection of solvent and metal counter-ion, …
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I. Enthalpy of Protonation Studies on Selected Organolithium Compounds. Ii. Dipole Stabilized Carbanions in N-Methyl Carboxamides
Made available in DSpace on 2014-12-13T20:10:04Z (GMT). No. of bitstreams: 1 7714930.pdf: 5080318 bytes, checksum: cf7b65bfc5e248c32aa17b9119ac4f66 (MD5) Previous issue date: 1977
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Intermolecular and intramolecular asymmetric induction at the beta-benzylic position of carboxamides in directed lithiation-substitution sequences
… at the $\beta$-benzylic position of secondary carboxamides in directed lithiation-substitution reactions has been achieved intermolecularly by using ($-$)-sparteine as the external chiral ligand and intramolecularly by using $\alpha$-methylbenzylamine as the covalently attached chiral auxiliary.
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Synthetic and spectroscopic studies of 6-substituted chromone derivatives
… in the chromone moiety of several chromone-2-carboxamides. The compounds synthesized were purified either by flash chromatography or recrystallization using ethanol-water. The yields of chromone-2-carboxylic acids ranged from 85-90 %, those of the chromone-2-carboxamides ranged from 40-72 %, …
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Metal ion complexation, extraction and transport by crown and lariat ether compounds
… variation within N-(R) sulfonyl lariat ether carboxamides upon the extraction efficiency and selectivity was explored in solvent competitive extraction. Very high Na* selectivity and extraction efficiency were achieved for N-(R)sulfonyl sym-(alkyl)dibenzo-16-crown-5-oxyacetamides. …
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Phosphodiesterase 4 inhibitors for the treatment of inflammation associated with respiratory disease
… sulphonamides, quinolones, 7-methoxybenzofuran-4-carboxamides, and 7-methoxyfuro[2,3-c]pyridine-4-carboxamides. The lead molecules selected in each publication had improved PDE4:RBA ratios which translated into an improved therapeutic window in vivo. These generated lead molecules (compound …
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SÍNTESE DE NOVOS POTENCIAIS ANTAGONISTAS DO NMDA SUBTIPO NR2B DO SISTEMA NERVOSO CENTRAL BASEADOS EM CARBOXAMIDAS TRIAZÓLICAS
… as intermediates in the syntheses of new amino carboxamides with potentials antagonistic activities of the N-methyl-D-aspartate in the central nervous system. While the 3-amine-5-trifluoromethyl-2H-1,2,4-triazole (2) was prepared in one step starting from the trifluoroacetic acid, the …
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Synthetic studies and biological evaluation of chromone - 3 - carbaldehydes
… acids. A series of chromone-3-carboxamides was obtained from corresponding 4-oxo-4H-chromene-3-carboxylic acid via the in situ generation of the corresponding acid chloride in good yield. The second class of compounds were achieved by reacting corresponding …
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Synthesis, Characterization, And Self-Assembly Of Bi-Carbamates And Tri-Carbamates
… study, a number of two-armed and three-armed carboxamides and carbamates have been synthesized, characterized and self-assembly process was studied. The self-assembly of these amides and carbamates were studied in a large number of single solvents as well as combination of solvents. Two-armed …
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Studies in the synthesis and analysis of novel heterocyclic synthetic cannabinoid receptor agonists
… for the synthesis of pyrazolopyridine-3-carboxamides and presents the first reported spectroscopic discussion of azaindazole-type SCRA NPS.
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Synthesis of 6-Substitutedchromone-2- Carboxamide derivatives as corrosion inhibitors for metals in acidic medium
… and inexpensive 6-substitutedchromone-2-carboxamides derivatives (Chromone-2-carboxamide, 6-bromochromone-2-carboxamide, 6-chlorochromone-2-carboxamide, 6-methoxychromone-2-carboxamide and 6-nitrochromone-2-carboxamide) were successful synthesized and evaluated as potential corrosion …
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Studies into the Biosynthesis and Chemical Synthesis of Indolocarbazoles and Related Heterocyclic Compounds. Metalation of Indole-6-Carboxamide.
… and C-7 indole metalation tactics of indole-6-carboxamides, in order to provide new functionalized indoles. The use of an indole C-2 silicon protection strategy in combination with a sterically bulky C-6 N,N-di-isopropyl carboxamide directed metalation group overcame undesired side reactions …
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STRUCTURE–ACTIVITY RELATIONSHIP STUDIES OF HYBRID ANTITUMOR AGENTS FOR THE TREATMENT OF NON-SMALL CELL LUNG CANCER
… thiourea- and guanidine-modified acridine-4-carboxamides and a corresponding platinum–intercalator conjugate have been synthesized and evaluated as cytotoxic agents. The point of attachment of the platinum-modified linker was changed from the 9-position to the 4-position of acridine to alter …
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Antimalarial Agents: New Mechanisms of Actions for Old and New Drugs
… library of γ- substituted oxoisoxazole- 2(3H)-carboxamides and isoxazol-3-yl carbamates, and nitriles as AChE inhibitors targeting wild- type (G3) and resistant (Akron) An. gambiae mosquito. In total 23 compounds were synthesized and evaluated. Both carbamates and carboximides with a …
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The Chemical Synthesis of Model Catalysts Related to Enzymes
… anhydride method. Dehydrations of α-acylamino carboxamides to nitriles had never been reported in the chemical literature. The usual reagents for amide dehydrations failed; only phosphorous oxychloride in pyridine could be used successfully. The nitrile was then treated with dry hydrogen …
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