Archivo de la categoría: 2013

Coppola et al. Org Lett. 2013;15(13):3388-91. Remote aryl cyanation via isocyanide-cyanide rearrangement on tosylmethyl isocyanide derivatives.

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Publicaciones > Coppola et al

Remote aryl cyanation via isocyanide-cyanide rearrangement on tosylmethyl isocyanide derivatives.

Departamento de Quimica Organica y Quimica Inorganica, Universidad de Alcala, 28871 - Alcala de Henares, Madrid, Spain.

Abstract

The reaction of alkyl tosylmethyl isocyanides and 2-bromobenzyl bromides in the presence of t-BuLi gives rise to a cascade reaction to give unexpected 2-substituted 2,3-dihydro-1H-indenimines which, upon treatment with t-BuOK, rearrange to 2-vinylbenzonitriles in high overall yields. This simple procedure represents a new approach to the synthesis of aromatic nitriles via isocyanide-cyanide interconversion.

Ramirez et al. Organic and Biomolecular Chemistry. 2013;11(41):7145 -7154. Synthesis of charged bis-heteroaryl donor-acceptor (D-A+) NLO-phores coupling (π-deficient-π-excessive) heteroaromatic rings.

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Publicaciones > Ramirez et al

Synthesis of charged bis-heteroaryl donor-acceptor (D-A+) NLO-phores coupling (π-deficient-π-excessive) heteroaromatic rings.

1. Departamento de Química Orgánica y Química Inorgánica, Universidad de Alcalá, 28871-Alcalá de Henares, Madrid, Spain.  2. Department of Chemistry, University of Leuven, Celestijnenlaan 200 D, 3001 Leuven, Belgium.  3. Departamento de Quimica Analitica, Quimica Fisica e Ingenieria Quimica, Universidad de Alcalá, 28871 Alcalá de Henares, Madrid, Spain.  4. IES Matarraña, 44580 Valderrobres, Teruel, Spain.

Resumen

Charged chromophores based on heteroaromatic cations were prepared by reaction of alkylazinium salts with N-heteroarylstannanes under Stille conditions. This approach provides easy access to potential single donor D-A+ chromophores in which the acceptor moiety A+ is the pyridinium cation and the donors are different π-excessive N-heterocycles. The β hyperpolarizabilities were measured in hyper-Rayleigh scattering experiments and the experimental data are supported by a theoretical analysis that combines a variety of computational procedures, including density functional theory and correlated Hartree-Fock-based methods. In some chromophores, the absence of a bridge between donor and acceptor fragments increases the NLO properties. © 2013 The Royal Society of Chemistry.

Deligeorgiev et al. Current Materials Science. 2013;6(2):81. Recent Patents on Materials Science. Fluorescent Dyes for Bio-Applications in the Patent Literature

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Publicaciones > G.-Deligeorgiev et al

Fluorescent Dyes for Bio-Applications in the Patent LiteratureFluorescent Dyes for Bio-Applications in the Patent Literature

Resumen

For life science research the fluorescent probes are essential tools and their use is continually increasing due to their low cost and higher sensitivity comparing other methods, and the capability for quantitative determination of bioanalytes. In this article the recent patents related to fluorescent probes for detection of nucleic acids, protein detection, bio-imaging, covalent labeling of amino groups, thiol groups, fluorescent dyes for detection of cations in bio-objects and chemiluminescent dyes are reviewed. The dyes applied in new and promptly developing research fields as fluorescence image-guided surgery, fluorescence bio-sensors, fluorescnent nanoparticles are also described. The future trends in the fluorescence bio-labeling are also addressed.

Sánchez et al. Bioorg. Med. Chem.. 2013;21(8):2370 -2378. Synthesis and evaluation of quinazoline derivatives as phosphodiesterase 7 inhibitors.

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Publicaciones > Sánchez et al

Synthesis and evaluation of quinazoline derivatives as phosphodiesterase 7 inhibitors.

1. Departamento de Quimica Orgánica, Universidad de Alcala, 28871 Alcalá de Henares, Madrid, Spain.  2. Almirall-Prodesfarma, Laureà Miró 408-410, 08980 Sant Felíu de Llobregat, Barcelona, Spain.  3. Centro Nacional de Referencia Sobre Contaminantes Orgánicos Persistentes (CNRCOP), Parque Científico Tecnológico, Universidad de Alcalá, C/Punto Net, 4, 28871 Alcalá de Henares, Madrid, Spain.  4. Pharma Mar S.A., Avda. De los Reyes, 1 Pol. Ind. La Mina-Norte, 28770 Colmenar Viejo, Madrid, Spain.

Resumen

The latest scientific findings concerning PDE7 and PDE4 inhibition suggest that selective small-molecule inhibitors of both enzymes could provide a novel approach to treat a variety of immunological diseases. In this context, we describe a new series of quinazoline derivatives from quinazolin-4-thiones which include a substituted biphenyl fragment. Some of these compounds show inhibitory potencies at sub-micromolar levels against the catalytic domain of PDE7. © 2013 Elsevier Ltd. All rights reserved.