323 resultados para Diamines -- Síntesi
Resumo:
La hibridació de les noves tecnologies amb la posada en escena, en obres i espais de representació, està obrint noves formes d'aproximació al fet dramatúrgic. Així s'ha esdevingut en la història del teatre sobre l'escriptura, l'escenografia o l'acció actoral. El que aquí volem tractar és com les tecnologies interactives poden representar un altre d'aquests moments d'inflexió. Aquest article parteix de l'experiència obtinguda en la direcció, juntament amb Montse Figueras, de la instal·lació Prometzeus presentada a la sala Muncunill de Terrassa el 2004. Una aproximació amateur en l’experimentació de noves dramatúrgies que feia ús de tecnologies audiovisuals interactives. Volem presentar una primera reflexió sobre la qüestió i exposar set d'aquestes possibles reformulacions. Set punts on les tecnologies interactives reformulen el llenguatge teatral.
Resumo:
Additions of lactams, imides, (S)-4-benzyl-1,3-oxazolidin-2-one, 2-pyridone, pyrimidine-2,4-diones (AZT derivatives), or inosines to the electron-deficient triple bonds of methyl propynoate, tert-butyl propynoate, 3-butyn-2-one, N-propynoylmorpholine, or N-methoxy-N-methylpropynamide in the presence of many potential catalysts were examined. DABCO and, second, DMAP appeared to be the best (highest reaction rates and E/Z ratios), while RuCl3, RuClCp*(PPh3)2, AuCl, AuCl(PPh3), CuI, and Cu2(OTf)2 were incapable of catalyzing such additions. The groups incorporated (for example, the 2-(methoxycarbonyl)ethenyl group that we name MocVinyl) serve as protecting groups for the above-mentioned heterocyclic CONH or CONHCO moieties. Deprotections were accomplished via exchange with good nucleophiles: the 1-dodecanethiolate anion turned out to be the most general and efficient reagent, but in some particular cases other nucleophiles also worked (e.g., MocVinyl-inosines can be cleaved with succinimide anion). Some structural and mechanistic details have been accounted for with the help of DFT and MP2 calculations.
Resumo:
Els avenços en el camp de la simulació estanmodificant i adaptant les necessitats de les professions sanitàries. Diversos estudis comparatius recolzen la necessitat de la simulació, demostrant ser la millor via per dotar d'habilitats i competències clíniques als professionals de ciències de la salut..L'Escola Universitària d'Infermeria (EUI) de la UB ofereix (2004/2013) dos cursos de Màster en Infermeria d'Urgències hospitalàries amb edicions presencial i semipresencial de 60 crèdits ECTS, adaptats als requisits docents i organitzatius de l'Espai Europeu d'Educació Superior (EEES).Aquests cursos incorporen un mòdul de 35 crèdits sobre el maneig del pacient crític a urgències. Al final d'aquest mòdul i com a síntesi d'aquests coneixements s'incorpora un taller d'alta simulació sobre el maneig de casos de pacient crítics en l'àmbit d'un àrea de crítics d'urgències.
Resumo:
L’article presenta una síntesi de les principals conclusions sobre Menors Migrants No Acompanyats, les seves característiques, els perfils existents i la invisibilitat social que els afecta no només com immigrants sinó també com a menors d’edat. Conclusions extretes de la investigació estatal realitzada sobre aquests i aquestes menors pel Grup d’Investigació IFAM (Infància i Família en Ambients Multiculturals). D’aquesta manera s’aporta informació descriptiva sobre aquest fenomen migratori, però també apunts per a la reflexió. S’inclou la perspectiva de gènere com a via per visibilitzar les menors de les quals menys coneixement es disposa al món acadèmic i a la societat en general.
Resumo:
A new approach to the synthesis of 4,5-disubstituted cyclopentenones is described. The strategy is based on the Pauson-Khand (PK) reaction of norbornadiene and N-Boc-propargylamine as alkyne with a masked leaving group, which can be eliminated at will. This approach to the synthesis of 4,5-disubstituted cyclopentenones overcomes the problem of using the alkylation to introduce the alpha-side-chain. As an example, prostane 13-epi-12-oxo-phytodienoic acid (13-epi-12-oxo-PDA) methyl ester was synthesized.
Resumo:
Síntesi dels primers resultats del Projecte Ager Tarraconensis i de les aportacions al simposi, de les quals s’extreuen reflexions i coneixements nous sobre el tema de l’estudi entorn del conjunt de l’espai de la ciutat romana, del paisatge, tractat com un sistema. Les aportacions se centren en la varietat de les primeres estratègies de control romà del territori, de les tipologies i evolució dels establiments, dels aspectes econòmics i de la dinàmica del poblament. Tot plegat fa referència molt especialment al territori de Tarraco, per bé que es fan nombroses comparacions amb altres territoris de l’àrea catalana i saguntina i també d’altres províncies romanes. Tarraco es va perfilant com una ciutat amb un territorium molt productiu, no sols en agricultura, sinó també en indústries, producció tèxtil, explotacions de recursos minerals com les pedreres i el ferro, i amb un comerç molt actiu que la devia convertir en un port important de la Mediterrània occidental romana. La jerarquia dels hàbitats rurals també s’està demostrant més complexa gràcies al coneixement de noves aglomeracions. L’evolució posterior al període romà també ha entrat en discussió, especialment pel que fa a l’època islàmica, sobre la qual es discuteix si el camp va quedar poblat o despoblat, tema que resol en sentit positiu el diagrama pol·línic realitzat dins del marc del projecte.
Resumo:
A new approach to the synthesis of 4,5-disubstituted cyclopentenones is described. The strategy is based on the Pauson-Khand (PK) reaction of norbornadiene and N-Boc-propargylamine as alkyne with a masked leaving group, which can be eliminated at will. This approach to the synthesis of 4,5-disubstituted cyclopentenones overcomes the problem of using the alkylation to introduce the alpha-side-chain. As an example, prostane 13-epi-12-oxo-phytodienoic acid (13-epi-12-oxo-PDA) methyl ester was synthesized.
Resumo:
Additions of lactams, imides, (S)-4-benzyl-1,3-oxazolidin-2-one, 2-pyridone, pyrimidine-2,4-diones (AZT derivatives), or inosines to the electron-deficient triple bonds of methyl propynoate, tert-butyl propynoate, 3-butyn-2-one, N-propynoylmorpholine, or N-methoxy-N-methylpropynamide in the presence of many potential catalysts were examined. DABCO and, second, DMAP appeared to be the best (highest reaction rates and E/Z ratios), while RuCl3, RuClCp*(PPh3)2, AuCl, AuCl(PPh3), CuI, and Cu2(OTf)2 were incapable of catalyzing such additions. The groups incorporated (for example, the 2-(methoxycarbonyl)ethenyl group that we name MocVinyl) serve as protecting groups for the above-mentioned heterocyclic CONH or CONHCO moieties. Deprotections were accomplished via exchange with good nucleophiles: the 1-dodecanethiolate anion turned out to be the most general and efficient reagent, but in some particular cases other nucleophiles also worked (e.g., MocVinyl-inosines can be cleaved with succinimide anion). Some structural and mechanistic details have been accounted for with the help of DFT and MP2 calculations.
Resumo:
The first total synthesis of Aeruginazole A, prepared via a convergent strategy that involved both solid-phase peptide synthesis and solution phase chemistry and that enabled conservation of the stereochemistry of the intermediates, is reported.
Resumo:
The synthesis of various polycyclic systems containing a C3aNi bond between a hexahydropyrrolo[2,3-b]indole and an indole tryptophan is described here. A series of experiments were performed to determine the best combination of five orthogonal protecting groups and the best reaction conditions for formation of said bond, which is a common feature among many recently discovered marine natural products.
Resumo:
A series of 1,2,3,4-tetrahydrobenzo[h][1,6]naphthyridines differently substituted at positions 1, 5, and 9 have been designed from the pyrano[3,2-c]quinoline derivative 1, a weak inhibitor of acetylcholinesterase (AChE) with predicted ability to bind to the AChE peripheral anionic site (PAS), at the entrance of the catalytic gorge. Fourteen novel benzonaphthyridines have been synthesized through synthetic sequences involving as the key step a multicomponent Povarov reaction between an aldehyde, an aniline and an enamine or an enamide as the activated alkene. The novel compounds have been tested against Electrophorus electricus AChE (EeAChE), human recombinant AChE (hAChE), and human serum butyrylcholinesterase (hBChE), and their brain penetration has been assessed using the PAMPA-BBB assay. Also, the mechanism of AChE inhibition of the most potent compounds has been thoroughly studied by kinetic studies, a propidium displacement assay, and molecular modelling. We have found that a seemingly small structural change such as a double O → NH bioisosteric replacement from the hit 1 to 16a results in a dramatic increase of EeAChE and hAChE inhibitory activities (>217- and >154-fold, respectively), and in a notable increase in hBChE inhibitory activity (> 11-fold), as well. An optimized binding at the PAS besides additional interactions with AChE midgorge residues seem to account for the high hAChE inhibitory potency of 16a (IC50 = 65 nM), which emerges as an interesting anti-Alzheimer lead compound with potent dual AChE and BChE inhibitory activities.
Resumo:
A series of 1,2,3,4-tetrahydrobenzo[h][1,6]naphthyridines differently substituted at positions 1, 5, and 9 have been designed from the pyrano[3,2-c]quinoline derivative 1, a weak inhibitor of acetylcholinesterase (AChE) with predicted ability to bind to the AChE peripheral anionic site (PAS), at the entrance of the catalytic gorge. Fourteen novel benzonaphthyridines have been synthesized through synthetic sequences involving as the key step a multicomponent Povarov reaction between an aldehyde, an aniline and an enamine or an enamide as the activated alkene. The novel compounds have been tested against Electrophorus electricus AChE (EeAChE), human recombinant AChE (hAChE), and human serum butyrylcholinesterase (hBChE), and their brain penetration has been assessed using the PAMPA-BBB assay. Also, the mechanism of AChE inhibition of the most potent compounds has been thoroughly studied by kinetic studies, a propidium displacement assay, and molecular modelling. We have found that a seemingly small structural change such as a double O → NH bioisosteric replacement from the hit 1 to 16a results in a dramatic increase of EeAChE and hAChE inhibitory activities (>217- and >154-fold, respectively), and in a notable increase in hBChE inhibitory activity (> 11-fold), as well. An optimized binding at the PAS besides additional interactions with AChE midgorge residues seem to account for the high hAChE inhibitory potency of 16a (IC50 = 65 nM), which emerges as an interesting anti-Alzheimer lead compound with potent dual AChE and BChE inhibitory activities.
Resumo:
We have synthesized a family of rheinhuprine hybrids to hit several key targets for Alzheimer"s disease. Biological screening performed in vitro and in Escherichia coli cells has shown that these hybrids exhibit potent inhibitory activities against human acetylcholinesterase butyrylcholinesterase, and BACE-1, dual Aβ42 and tau anti-aggregating activity, and brain permeability. Ex vivo studies with the leads (+)- and ()-7e in brain slices of C57bl6 mice have revealed that they efficiently protect against the Aβ-induced synaptic dysfunction , preventing the loss of synaptic proteins and/or have a positive effect on the induction of long term potentiation. In vivo studies in APP-PS1 transgenic mice treated i.p. for 4 weeks with (+)- and ()-7e have shown a central soluble Aβ lowering effect, accompanied by an increase in the levels of mature amyloid precursor protein (APP). Thus, (+)- and ()-7e emerge as very promising disease-modifying anti-Alzheimer drug candidates.
Resumo:
We have synthesized a family of rheinhuprine hybrids to hit several key targets for Alzheimer"s disease. Biological screening performed in vitro and in Escherichia coli cells has shown that these hybrids exhibit potent inhibitory activities against human acetylcholinesterase butyrylcholinesterase, and BACE-1, dual Aβ42 and tau anti-aggregating activity, and brain permeability. Ex vivo studies with the leads (+)- and ()-7e in brain slices of C57bl6 mice have revealed that they efficiently protect against the Aβ-induced synaptic dysfunction , preventing the loss of synaptic proteins and/or have a positive effect on the induction of long term potentiation. In vivo studies in APP-PS1 transgenic mice treated i.p. for 4 weeks with (+)- and ()-7e have shown a central soluble Aβ lowering effect, accompanied by an increase in the levels of mature amyloid precursor protein (APP). Thus, (+)- and ()-7e emerge as very promising disease-modifying anti-Alzheimer drug candidates.
Resumo:
For the first time, an enantioselective synthesis of both 1R,4S-isagarin 1a and 1S,4R-isagarin 1b was achieved starting from 1,4-dimethoxy-2-vinylnaphtalene 2. The key steps involve a Sharpless asymmetric dihydroxylation and reaction with an acetonylating pyridinium ylid.