Examinar por departamento (eus.) "Kimika organikoa I"
Now showing items 61-80 of 208
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Design and synthesis of novel topoisomerase I Inhibitors. 1,5-Naphthyridine derivatives with antiproliferative activity
(2016-07-21)El trabajo de investigación que se recoge en la presente memoria se ha centradoen el diseño y la síntesis de derivados de 1,5-naftiridinas con posible actividadbiológica como inhibidores de topoisomerasa I (TopI). La TopI ... -
Design and synthesis of quasi-diastereomeric molecules with unchanging central, regenerating axial and switchable helical chirality via cleavage and formation of Ni(II)–O and Ni(II)–N coordination bonds
(Beilstein Institut, 2012-11-13)We describe herein the design and synthesis of asymmetric, pentadentate ligands, which are able to coordinate to Ni(II) cations leading to quasi-diastereomeric complexes displaying two new elements of chirality: stereogenic ... -
Design, chemical synthesis and biological evaluation of new synthetic conjugates of ursodeoxycholic acid for the inhibition of cystogenesis in experimental models of polycystic liver disease.
(2019-11-05)Antecedentes y objetivos: Las enfermedades hepáticas poliquísticas (PLD) son un grupo heterogéneo de trastornos genéticos hereditarios caracterizados por el desarrollo progresivo de múltiples quistes biliares llenos de ... -
Detrifluoroacetylative in Situ Generated Cyclic Fluorinated Enolatesfor the Preparation of Compounds Featuring a C−F StereogenicCenter
(American Chemical Society, 2019-11-26)Practical methods for the preparation of selectively fluorinated compounds are in extremely high demand in nearly every sector of the pharmaceutical and agrochemical industries. Here we provided an account of the recent ... -
Development of an α’-hydroxy enone for the aminocatalytic asymmetric formal conjugate addition of aldehydes to acrylates, vinyl ketones and acrolein
(Royal Society of Chemistry, 2023-05-24)Aminocatalytic asymmetric conjugate addition of aldehydes to Michael acceptors is a well established C–C bond forming methodology. However, various acrylic-type acceptors, including acrylic acid derivatives and acrolein, ... -
Development of Hamari Ligands for Practical Asymmetric Synthesisof Tailor-Made Amino Acids
(American Chemical Society, 2019-11-19)Enantiomerically pure tailor-made amino acids are in extremely high demand in nearly every sector of the health-related industries. In particular, the rapidly growing number of amino-acid-based pharmaceuticals calls for ... -
Development of novel hybrid phosphorated quinoline derivatives as topoisomerase 1B inhibitors with antiproliferative activity
(2022-07-07)El presente trabajo de Tesis Doctoral recopila la síntesis y evaluación biológica de nuevos derivados híbridos de quinolinas fosforadas como inhibidores de topoisomerasa 1B humana (hTOP1B) con actividad antiproliferativa. ... -
Diastereoselective ZnCl2-Mediated Joullié–Ugi Three-Component Reaction for the Preparation of Phosphorylated N-Acylaziridines from 2H-Azirines
(MDPI, 2024-02-27)We disclose a direct approach to the diastereoselective synthesis of phosphorus substituted N-acylaziridines based on a one-pot ZnCl2-catalyzed Joullié–Ugi three-component reaction of phosphorylated 2H-azirines, carboxylic ... -
Diethyl(benzamido(diisopropoxyphosphoryl)methyl) phosphonate
(MDPI, 2022-08-11)Bisphosphonates are widely used in medicine and related areas, mainly for the treatment of bone diseases, such as osteoporosis. However, their synthesis is usually performed under harsh reaction conditions. In order to ... -
Direct Enantioselective Michael Reactions of Ketones and Aldehydes with Nitroalkenes under Brønsted Base/H-Bonding Catalysis
(2020-12-03)promover la a-funcionalización directa y enantioselectiva de cetonas y aldehídos con ciertascaracterísticas estructurales. Específicamente, en esta Tesis Doctoral se ha estudiado la reacción deMichael enantioselectiva de ... -
Diseño y evaluación de nuevos derivados de aziridinas fosforadas como agentes
(2021-03-26)Esta Tesis Doctoral, tiene como objetivo principal la síntesis de nuevos derivados de aziridina fosforados y su estudio como agentes antiproliferativos. Esta memoria se fundamenta en 4 objetivos principales, algunos de los ... -
Diseño, síntesis, caracterización y evaluación biológica y conformacional de peptidomiméticos y depsipeptidomiméticos b-lactámicos: Una nueva generación de inhibidores de la integrina avb3.
(2016-07-01)En la presente Tesis Doctoral se describe el diseño, la síntesis, la caracterización y la evaluación biológica y conformacional de una biblioteca de peptidomiméticos y depsipeptidomiméticos, tanto cíclicos como de cadena ... -
DoE-driven development of an organocatalytic enantioselective addition of acetaldehyde to nitrostyrenes in water
(Wiley-VCH, 2022-03-01)Moving from organic solvents to water is not always an easy task, especially when a lot of variables need to be screened. The development of an enantioselective enamine-catalysed Michael addition of acetaldehyde to ... -
Dynamic Nucleophilic Aromatic Substitution of Tetrazines
(Wiley, 2021-08-23)A dynamic nucleophilic aromatic substitution of tetrazines (SNTz) is presented herein. It combines all the advantages of dynamic covalent chemistry with the versatility of the tetrazine moiety. Indeed, libraries of compounds ... -
Efficient AntiMycolata Agents by Increasing the Lipophilicity of Known Antibiotics through Multicomponent Reactions
(MDPI, 2023-01-03)New antibiotic agents were prepared using Povarov and Ugi multicomponent reactions upon the known drugs sulfadoxine and dapsone. The prepared derivatives, with increased lipophilicity, showed improved efficiency against ... -
Enantioselective Addition of Alkynyl Ketones to Nitroolefins Assisted by Bronsted Base/H-Bonding Catalysis
(Wiley, 2019-03-21)Various sets of enolizable alkynyl ketones (including methyl ynones with α-aryl, α-alkenyl, and α-alkoxy groups) were able to react smoothly with nitroolefins with the assistance of bifunctional Brønsted base/H-bond catalysts ... -
Enantioselective Construction of Tetrasubstituted Stereogenic Carbons through Brønsted Base Catalyzed Michael Reactions: α´-Hydroxy Enones as Key Enoate Equivalent
(ACS, 2014-11-25)Catalytic and asymmetric Michael reactions constitute very powerful tools for the construction of new C–C bonds in synthesis, but most of the reports claiming high selectivity are limited to some specific combinations of ... -
Enantioselective Michael Addition of Aldehydes to Maleimides Organocatalyzed by a Chiral Primary Amine-Salicylamide
(MDPI, 2018-12-12)A primary amine-salicylamide derived from chiral trans-cyclohexane-1,2-diamine was used as an organocatalyst for the enantioselective conjugate addition of aldehydes, mainly ,-disubstituted to N-substituted maleimides. The ... -
Enantioselective synthesis of a-aminophosphonic acid derivatives.
(2019-11-25)Los ácidos -aminofosfónicos y sus derivados son estructuras muy frecuentes en productos con alto interés biológico como fármacos y agroquímicos.Durante las últimas décadas, el elevado interes de la industria en derivados ... -
Enhancing Dual-State Emission in Maleimide Fluorophores through Fluorocarbon Functionalisation
(Wiley, 2022-10)Herein, a library of trifluoroethyl substituted aminomaleimide derivatives are reported with small size and enhanced emissions in both solution and solid-state. A diCH2CF3 substituted aminochloromaleimide exhibits the most ...