Electrophilically Activated Nitroalkanes in Synthesis of 3,4-Dihydroquinozalines

Nitroalkanes activated with polyphosphoric acid serve as efficient electrophiles in reactions with various nucleophilic amines. Strategically placed second functionality allows for the design of annulation reactions enabling preparation of various heterocycles. This strategy was employed to develop an innovative synthetic approach towards 3,4-dihydroquinazolines from readily available 2-(aminomethyl)anilines

Synthesis of imidazo[1,5-a]pyridines via cyclocondensation of 2-(aminomethyl)pyridines with electrophilically activated nitroalkanes

Imidazo[1,5-a]pyridines were efficiently prepared via the cyclization of 2-picolylamines with nitroalkanes electrophilically activated in the presence of phosphorous acid in polyphosphoric acid (PPA) medium

A Convenient Way to Quinoxaline Derivatives through the Reaction of 2-(3-Oxoindolin-2-yl)-2-phenylacetonitriles with Benzene-1,2-diamines

Microwave-assisted reaction between 2-(3-oxoindolin-2-yl)-2-phenylacetonitriles andbenzene-1,2-diamines leads to the high-yielding formation of the corresponding quinoxalines as sole, easily isolaable products. The featured transformation involves unusual extrusion of phenylacetonitrile molecule and could be performed in a short sequence starting from commonly available indoles and nitroolefins

Improved Method for Preparation of 3-(1H-Indol-3-yl)benzofuran-2(3H)-ones

3-(1H-Indol-3-yl)benzofuran-2(3H)-ones were efficiently accessed via polyphosphoric acid-mediated condensation of 3-(2-nitrovinyl)-1H-indoles with phenols

Process for Enhancing the Activity of Amyloid β Peptides

A novel process for enhancing activity of an oligopeptide or polypeptide comprising the steps of: providing an oligopeptide or polypeptide, dissolving the oligopeptide or polypeptide in an organic solvent, heating, removing the solvent, and recovering an oligopeptide or polypeptide with enhanced activity is disclosed. Also disclosed are novel oligopeptides and polypeptides enhanced by the process according the invention

Metal-free transannulation reaction of indoles with nitrostyrenes: a simple practical synthesis of 3-substituted 2-quinolones

3-Substituted 2-quinolones are obtained via a novel, metal-free transannulation reaction of 2-substituted indoles with 2-nitroalkenes in polyphosphoric acid. The reaction can be used in conjunction with the Fisher indole synthesis offering a practical three-component heteroannulation methodology to produce 2-quinolones from arylhydrazines, 2-nitroalkenes and acetophenone

The antioxidant vitamin E modulates amyloid b-peptid-induced creatine kinase activity inhibition and increased protein oxidation: Implications for the free radical hypothesis of Alzheimer’s disease

Amyloid B-peptide (AB), the main constituent of senile plaques in Alzheimer's disease (AD) brain, is hypothesized to be a key factor in the neurodegeneration seen in AD. Recently it has been shown by us and others that the neurotoxicity of AB occurs in conjunction with free radical oxidative stress associated with the peptide. AB(1-40) and several other fragments of the AB sequence are associated with free radicals in solution that are detectable using electron paramagnetic resonance spectroscopy. These free radicals were shown to attack brain cell membranes, initiate lipid peroxidation, increase Ca 2+ influx and damage membrane and cytosolic proteins. In AD brain obtained under rapid autopsy protocol, the activity of the oxidatively-sensitive enzyme creatine kinase was shown to be significantly reduced. We reasoned that AB-associated free radical-induced modification of creatine kinase activity and other markers of cellular damage might be modulated by free radical scavengers. Accordingly, this study demonstrates that vitamin E can modulate AB(25-35)-induced oxidative damage to creatine kinase and cellular proteins in cultured embryonic hippocampal neurons. These results, consistent with the hypothesis of free radical-mediated AB toxicity in AD, are discussed with deference to potential free radical scavengers as therapeutic agents for slowing the progression of AD

The Blackholic energy and the canonical Gamma-Ray Burst IV: the "long", "genuine short" and "fake - disguised short" GRBs

(Shortened) [...] After recalling the basic features of the "fireshell model", we emphasize the following novel results: 1) the interpretation of the X-ray flares in GRB afterglows as due to the interaction of the optically thin fireshell with isolated clouds in the CircumBurst Medium (CBM); 2) an interpretation as "fake - disguised" short GRBs of the GRBs belonging to the class identified by Norris & Bonnell [...] consistent with an origin from the final coalescence of a binary system in the halo of their host galaxies with particularly low CBM density [...]; 3) the first attempt to study a genuine short GRB with the analysis of GRB 050509B, that reveals indeed still an open question; 4) the interpretation of the GRB-SN association in the case of GRB 060218 via the "induced gravitational collapse" process; 5) a first attempt to understand the nature of the "Amati relation", a phenomenological correlation between the isotropic-equivalent radiated energy of the prompt emission E_{iso} with the cosmological rest-frame \nu F_{\nu} spectrum peak energy E_{p,i}. In addition, recent progress on the thermalization of the electron-positron plasma close to their formation phase, as well as the structure of the electrodynamics of Kerr-Newman Black Holes are presented. An outlook for possible explanation of high-energy phenomena in GRBs to be expected from the AGILE and the Fermi satellites are discussed. As an example of high energy process, the work by Enrico Fermi dealing with ultrarelativistic collisions is examined. It is clear that all the GRB physics points to the existence of overcritical electrodynamical fields. In this sense we present some progresses on a unified approach to heavy nuclei and neutron stars cores, which leads to the existence of overcritical fields under the neutron star crust.Comment: 68 pages, 50 figures, in the Proceedings of the XIII Brazilian School on Cosmology and Gravitation, M. Novello, S.E. Perez-Bergliaffa, editor