- One-Pot Metal-Free Cascade Synthesis of 2-(Perfluoroalkyl)pyrroles
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An efficient synthesis of 2-(perfluoroalkyl)pyrroles that employs a sequential one-pot three-component reaction between substituted ω-bromoacetophenones, anilines, and methyl perfluoroalk-2-ynoates has been developed. This transition-metal-free cascade pr
- Sun, Xuechun,Han, Jing,Chen, Jie,Deng, Hongmei,Shao, Min,Zhang, Hui,Cao, Weiguo
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supporting information
p. 7086 - 7090
(2015/11/16)
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- A concise formation of N-substituted 3,4-diarylpyrroles-synthesis and cytotoxic activity
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A short synthesis of N-substituted 3,4-diarylpyrroles by condensation of a phenacyl halide with a primary amine and a phenylacetaldehyde is reported. The key step is an intramolecular cyclization of an in situ generated enamine onto a ketone. Using differently substituted aromatic reactants and N-(3-aminopropyl)azatricyclodecane as the amine component, the preparation of analogs of the cytotoxic marine alkaloid halitulin could be achieved. The cytotoxicity of some of the compounds obtained by this method was studied, and one of them proved to be a very potent derivative, acting at a nanomolar concentration, in a caspase-independent cell death mechanism.
- Egorov, Maxim,Delpech, Bernard,Aubert, Genevieve,Cresteil, Thierry,Garcia-Alvarez, Maria Concepcion,Collin, Pascal,Marazano, Christian
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supporting information
p. 1518 - 1524
(2014/03/21)
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- Synthesis and 2D QSAR of O-sulphonated β-aminols derivatives as novel antifungal and antibacterial agents
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Synthesis of a series of b-aminol derivatives using regioselective opening reaction catalyzed by SiO2 (60-120 mesh) and O-sulphonation in THF-KOH system, comprising tert-butoxycarbonyl at secondary nitrogen and evaluate for various stains of bacteria and fungi. SAR study of synthesized compound using backward regression analysis.
- Saxena, Anil K.,Sharma, Sugandha,Pandey, Atindra K.,Shukla, Praveen K.
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p. 6476 - 6481
(2011/11/29)
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- Regiospecific and highly flexible synthesis of 1,4,5-trisubstituted 2-sulfanylimidazoles from structurally diverse ethanone precursors
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Imidazoles represent important bioactive scaffolds in medicinal chemistry. More than 2,500 structures are listed in drug discovery databases and over 3,000 patents have been claimed for imidazole-based structures. Recent imidazole pharmacophores have targ
- Laufer, Stefan A.,Hauser, Dominik R. J.,Liedtke, Andy J.
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p. 253 - 266
(2008/12/22)
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- Photolysis of α-azidoacetophenones: Trapping of triplet alkyl nitrenes in solution
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(Matrix presented) Selective excitation of the ketone chromophore in α-azidoacetophenones, 1, leads to intramolecular triplet energy transfer to the azido group, which forms the corresponding triplet alkyl nitrene, 2. Azides 1 also undergo α-cleavage to form benzoyl and methyl azido radicals in competition with nitrene formation. Thus the major photoproduct, 2-benzoylamino-1-phenylethanone, 3, comes from trapping of 2 with a benzoyl radical. This appears to be the first observation of bimolecular trapping of triplet alkyl nitrenes in solution.
- Mandel, Sarah M.,Bauer, Jeanette A. Krause,Gudmundsdottir, Anna D.
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p. 523 - 526
(2007/10/03)
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- Enantioselective synthesis of β-hydroxy amines and aziridines using asymmetric transfer hydrogenation of α-amino ketones
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Enantioselective transfer hydrogenation of α-amino ketones is an effective method for the asymmetric synthesis of β-hydroxy amines and aziridines.
- Kawamoto,Wills
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p. 1916 - 1928
(2007/10/03)
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- Enantioselective synthesis of β-hydroxy amines and aziridines using asymmetric transfer hydrogenation of α-amido ketones
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A rapid, expedient and enantioselective method for the synthesis of β-hydroxy amines and monosubstituted aziridines in up to 99% e.e., via asymmetric transfer hydrogenation of α-amido ketones, is described. Copyright (C) 2000 Elsevier Science Ltd.
- Kawamoto, Aparecida,Wills, Martin
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p. 3257 - 3261
(2007/10/03)
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