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Facile preparation of 3-substituted 2-quinazolinones via electrogenerated base
10.1016/j.tet.2018.03.010 2018-03-07 A new series of 3,4-disubstituted quinazolin-2-ones, with potential T-type calcium channel antagonist activity, and new 4-methylene-quinazolin-2-ones, promising catalysts as N-heterocyclic olefins, have been prepared in good yield by a simple reaction between... |
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Proton transfer process in synthesis of 3-acetyl-4-(substituted ethylenyl)coumarins and chromeno[3,4-c]pyridines
10.1016/j.tet.2018.03.015 2018-03-07 The triphenylphosphine mediated reactions of electron-deficient carbon-carbon triple bonds with 3-acetylcoumarins in dichloromethane afford functionalized 3-acetyl-4-(substituted ethylenyl)coumarins. Also, triphenylphosphine-catalyzed three-component cascade ... |
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Facile synthesis of perfluoroalkylated fluorenes via a one-pot two-step three-component process
10.1016/j.tet.2018.03.012 2018-03-07 The efficient synthesis of perfluoroalkyl-substituted fluorenes directly from indenones, malononitrile and methyl perfluoroalk-2-ynoates via a one-pot two-step three-component cascade process is reported. Up to 12 examples of indenones with various substituen... |
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Isa‒NHC‒catalyzed intermolecular stetter reaction of aromatic aldehydes with maleimides: An efficient access to 3‒aroylsuccinimides
10.1016/j.tet.2018.03.009 2018-03-07 An intermolecular Stetter reaction of aromatic aldehydes with maleimides has been developed using thiazolylidene salt derived Isa‒NHC as an efficient organocatalyst. The synthesized Stetter products “3‒aroylsuccinimides” are important building blocks for the ... |
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Cembranoids from Eunicea sp. enhance insulin-producing cells proliferation
10.1016/j.tet.2018.03.011 2018-03-07 Nine new cembranoids 1–9 containing an α–methylene–γ–butyrolactone together with the known diterpenes 10–15 have been isolated from a crude extract of Eunicea sp. and their structures were established by spectroscopic methods. The proliferative effect of six ... |
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Design and synthesis of new carbohydrate-lithocholic acid conjugates linked via 1,2,3-triazole rings
10.1016/j.tet.2018.03.008 2018-03-07 In this work, we report the synthesis of a novel carbohydrate-lithocholic acid conjugate linked through of 1,2,3-triazole rings and its derivatives in good to excellent yields. The conjugate was synthesized via copper-catalyzed azide−alkyne cycloaddition (CuA... |
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Aminothiazoles and aminothiadiazoles as nucleophiles in aminocarbonylation of iodobenzene derivatives
10.1016/j.tet.2018.03.007 2018-03-06 Various 2-, 3- and 4-substituted iodobenzenes were aminocarbonylated using aminothiazole and aminothiadiazole derivatives in palladium-catalysed reaction. The reaction is chemospecific toward the corresponding carboxamides. Consequently, the application of th... |
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Copper-facilitated Suzuki-Miyaura coupling for the preparation of 1,3-dioxolane-protected 5-arylthiophene-2-carboxaldehydes
10.1016/j.tet.2018.03.001 2018-03-06 5-Formyl-2-thiopheneboronic acid is a widely used building block for the synthesis of diverse structures, however, due to a significant instability its transformation to 5-arylthiophene-2-carboxaldehydes by C-C couplings could be performed only in low yields.... |
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Total chemical synthesis of human thyroid-stimulating hormone (hTSH) β-subunit: Application of arginine-tagged acetamidomethyl (AcmR) protecting groups
10.1016/j.tet.2018.02.067 2018-03-06 The β-subunit of human thyroid stimulating hormone (hTSH) has been synthesized as a single glycoform bearing a chitobiose disaccharide at the native glycosylation site. Key to the successful completion of this synthesis was the introduction of an arginine-tag... |
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Direct synthesis of anthracenes from o-tolualdehydes and aryl iodides through Pd(II)-Catalyzed sp3 C  H arylation and electrophilic aromatic cyclization
10.1016/j.tet.2018.03.006 2018-03-06 The first direct synthesis of substituted anthracenes from o-tolualdehydes and aryl iodides via a Pd(II)-catalyzed C |