Broad‐Spectrum Antifungal Agents: Fluorinated Aryl‐ and Heteroaryl‐Substituted Hydrazones
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DOI: 10.1002/cmdc.202000626
Abstract: Fluorinated aryl‐ and heteroaryl‐substituted monohydrazones displayed excellent broad‐spectrum activity against various fungal strains, including a panel of clinically relevant Candida auris strains relative to a control antifungal agent, voriconazole (VRC). These monohydrazones displayed less hemolysis… read more here.
Keywords: spectrum antifungal; fluorinated aryl; heteroaryl substituted; aryl heteroaryl ... See more keywords
Quinazoline‐Directed C–H Bond Functionalization Catalyzed by Ruthenium(II) Carboxylate – Construction of Polyconjugated Aryl‐Heteroaryl Systems
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DOI: 10.1002/ejoc.201700097
Abstract: A series of coupling products have been prepared by a ruthenium(II)-catalyzed direct ortho-C–H arylation of 2-(aryl/heteroaryl)-substituted quinazolines with (hetero)aryl bromides. Tri(hetero)aryl-substituted alkenes were also prepared by olefinic C–H activation of 2-(2-arylvinyl)quinazoline derivatives. High conversions and… read more here.
Keywords: ruthenium; aryl heteroaryl; functionalization; ruthenium carboxylate ... See more keywords
3-Aryl/Heteroaryl-5-amino-1-(3',4',5'-trimethoxybenzoyl)-1,2,4-triazoles as antimicrotubule agents. Design, synthesis, antiproliferative activity and inhibition of tubulin polymerization.
Sign Up to like & getrecommendations! Published in 2018 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2018.06.037
Abstract: Many natural and synthetic substances are known to interfere with the dynamic assembly of tubulin, preventing the formation of microtubules. In our search for potent and selective antitumor agents, a novel series of 1-(3',4',5'-trimethoxybenzoyl)-5-amino-1,2,4-triazoles were… read more here.
Keywords: amino; trimethoxybenzoyl; aryl heteroaryl; tubulin ... See more keywords
N-heterocyclic carbene-palladium-imine complex catalyzed α-arylation of ketones with aryl and heteroaryl chlorides under air atmosphere
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DOI: 10.1016/j.tetlet.2020.152124
Abstract: Abstract A new structure of saturated ring skeleton monoligated NHC-Pd-Imine complex was easily synthesized and unambiguously confirmed by X-ray single crystal diffraction. It was found to be an efficient and air-stable catalyst for the α-arylation… read more here.
Keywords: imine complex; air atmosphere; air; arylation ketones ... See more keywords
Scandium Triflate-Catalyzed N-[18F]Fluoroalkylation of Aryl- Or Heteroaryl-Amines with [18F]Epifluorohydrin under Mild Conditions.
Sign Up to like & getrecommendations! Published in 2022 at "Organic letters"
DOI: 10.1021/acs.orglett.2c01459
Abstract: The scandium triflate-catalyzed N-[18F]fluoroalkylation of aryl- or heteroaryl-amines with [18F]epifluorohydrin ([18F]2) was investigated. This reaction is mild and provides one-step access to N-[18F]fluoroalkylated aryl- or heteroaryl-amines, which are used for positron emission tomography imaging. The… read more here.
Keywords: triflate catalyzed; scandium triflate; aryl heteroaryl; heteroaryl amines ... See more keywords
Bifunctional Oxo-Tethered Ruthenium Complex Catalyzed Asymmetric Transfer Hydrogenation of Aryl N-Heteroaryl Ketones.
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DOI: 10.1021/acs.orglett.7b00691
Abstract: A facile asymmetric transfer hydrogenation of ortho-substituted aryl N-heteroaryl ketones and non-ortho-substituted N-oxide of aryl N-heteroaryl ketones using a readily available oxo-tethered ruthenium complex as a catalyst and sodium formate as a hydrogen source in… read more here.
Keywords: heteroaryl ketones; transfer hydrogenation; asymmetric transfer; aryl heteroaryl ... See more keywords
Iridium-Catalyzed Highly Enantioselective Transfer Hydrogenation of Aryl N-Heteroaryl Ketones with N-Oxide as a Removable ortho-Substituent.
Sign Up to like & getrecommendations! Published in 2018 at "Organic letters"
DOI: 10.1021/acs.orglett.7b03878
Abstract: A highly enantioselective transfer hydrogenation of non-ortho-substituted aryl N-heteroaryl ketones, using readily available chiral diamine-derived iridium complex (S,S)-1f as a catalyst and sodium formate as a hydrogen source in a mixture of H2O/i-PrOH (v/v =… read more here.
Keywords: heteroaryl ketones; transfer hydrogenation; enantioselective transfer; oxide removable ... See more keywords
1,1-Difluoro-3-aryl(heteroaryl)-1H-pyrido[1,2-c][1,3,5,2]oxadiazaborinin-9-ium-1-uides: synthesis; structure; and photophysical, electrochemical, and BSA-binding studies
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DOI: 10.1039/c7nj04032f
Abstract: This paper presents a series of six examples of 1,1-difluoro-3-aryl(heteroaryl)-1H-pyrido[1,2-c][1,3,5,2]oxadiazaborinin-9-ium-1-uides (2)—in which aryl(heteroaryl) = phenyl, 4-MeC6H4, 4-N(CH3)2C6H4, 4-NO2C6H4, 2-naphthyl, and 2-thienyl—as pyridine-based boron heterocycles with variable ligand structures. The heterocycles 2 were easily synthesized at… read more here.
Keywords: heteroaryl; oxadiazaborinin ium; difluoro aryl; pyrido oxadiazaborinin ... See more keywords
Nickel-Catalyzed Electrochemical Reductive Homocouplings of Aryl and Heteroaryl Halides: A Useful Route to Symmetrical Biaryls
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DOI: 10.1055/s-0036-1589100
Abstract: Due to their widespread presence in functional materials and pharmaceuticals, biaryls are of fundamental importance in organic chemistry. Methods for the synthesis of symmetrical biaryls generally involve both metallic reduction and transition-metal catalysis. In this… read more here.
Keywords: biaryls; symmetrical biaryls; aryl heteroaryl; heteroaryl halides ... See more keywords
Nickel-Catalyzed Cross-Coupling of Functionalized Organomanganese Reagents with Aryl and Heteroaryl Halides Promoted by 4-Fluorostyrene
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DOI: 10.1055/s-0036-1589101
Abstract: A catalytic system consisting of Ni(acac)2 (5 mol%) and 4-fluorostyrene (20 mol%) allows a convenient cross-coupling of functionalized organomanganese reagents with a variety of aryl and heteroaryl halides leading to polyfunctionalized diaryl- and arylheteroarylmethane derivatives. read more here.
Keywords: coupling functionalized; aryl heteroaryl; heteroaryl halides; nickel catalyzed ... See more keywords
Palladium-Catalyzed Synthesis of Aryl and Heteroaryl Difluoromethylated Phosphonates
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DOI: 10.1055/s-0036-1589140
Abstract: We report the palladium-catalyzed introduction of the difluoromethylposphonate unit onto aryl and heteroaryl iodides under mild conditions. Using the CuCF2PO(OEt)2 species generated in situ, the method allows the functionalization of various otherwise reluctant substrates. In… read more here.
Keywords: aryl heteroaryl; palladium catalyzed; catalyzed synthesis; synthesis aryl ... See more keywords