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Solvent-free microwave synthesis of novel 6-hydroxypyrimidin-4(1H)-one derivatives using arylmalonates

The disclosure herein describes the rapid synthesis of novel 6-hydroxypyrimidin-4(1H)-one derivatives via a solvent-free microwave cyclocondensation reaction using di-(2,4,6-trichlorophenyl)malonates and a variety of heterocyclic amines.

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Benzoxazole – Wikipedia,
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Flow hydrodediazoniation of aromatic heterocycles

Continuous flow processing was applied for the rapid replacement of an aromatic amino group with a hydride. The approach was applied to a range of aromatic heterocycles, confirming the wide scope and substituent-tolerance of the processes. Flow equipment was utilized and the process optimised to overcome the problematically-unstable intermediates that have restricted yields in previous studies relying on batch procedures. Various common organic solvents were investigated as potential hydride sources. The approach has allowed key structures, such as amino-pyrazoles and aminopyridines, to be deaminated in good yield using a purely organic-soluble system.

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Benzoxazole – Wikipedia,
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Pharmaceutical composition for prevention or treatment of pneumonia comprising dihydroquinoline carboxamide derivative or pharmacurically acceptable salt thereof as an active ingredient

Disclosed hereinafter calcium channel blockers carboxamide derivatives or pharmaceutically acceptable salts substituted active ingredient including medicinal compositions for the prevention or treatment of Streptococcus pneumoniae disclosure with each other. Said pharmaceutical compositions have a good antimicrobial activity as well as have, unlike conventional generally used such as erythromycin number having excellent antibacterial drug resistance by Streptococcus pneumoniae pneumonia germ pneumonia germ used in pharmaceutical compositions for the prevention or treatment of diseases is thus useful as can be used. (by machine translation)

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P-NITROPHENYL ACETATE HYDROLYSIS USING NUCLEOPHILIC CATALYSTS GRAFTED ON POLYMER-SUPPORTS

Two series of heterocyclic nucleophile polymer-grafted catalysts were prepared by polymer-analogous reactions. The catalysts were used in the p-nitrophenyl acetate hydrolysis. The kinetic study had confirmed that the reaction mechanism remain unchanged by grafting and characteristic for a nucleophilic catalysis.

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Benzoxazole – Wikipedia,
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Bis-(benzothiazol-2-yl)-amines and their metal amides: A structural comparison in the solid state

Within this work, the field of amide ligand platforms for group 13 metal complexation, especially for Al(iii) is investigated in a synthetic as well as in a structural comparative approach. Starting from bis-heterocyclo methanides, which mimic the omnipresent nacnac ligand, the next enhancement in this class of ligands includes the exchange of the central methylene bridge by an amine nitrogen atom. With this modification three different sec. amines, each symmetrically substituted, could be synthesised as parent neutral benzothiazole containing ligand systems: (NCSC6H4)2NH (1), (4-MeNCSC6H3)2NH (2) and (4-OMeNCSC6H3)2NH (3). Apart from these compounds also a lithiated species and a row of group 13 metal complexes of the deprotonated ligands could be examined by applying single crystal X-ray diffraction analyses. In this course three new dimethyl aluminium containing complexes [Me2Al{(NCSC6H4)2N}] (4), [Me2Al{(4-MeNCSC6H3)2N}] (5) and [Me2Al{(4-OMeNCSC6H3)2N}¡¤AlMe3] (6) as well as two lithiated compounds [Li{(NCSC6H4)2N}]4 (7), [Li{(4-MeNCSC6H3)2N}]4 (8) were structurally and spectroscopically characterised. A subsequent structural comparison of 1-6 and 8 in the solid state shows that the parent ligand systems prefer a planar cis-trans alignment due to hydrogen bond formation. In contrast to that, the metallated species favour a planar but trans-trans or cis-cis alignment depending on the metal cation.

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COMPOSITIONS COMPRISING A PI3K INHIBITOR AND AN HDAC INHIBITOR

The invention relates to a pharmaceutical composition comprising at least one PI3K inhibitor of Formula I or a pharmaceutically acceptable salt thereof and at least one HDAC inhibitor such as a compound of Formula II or a pharmaceutically acceptable salt thereof; or at least one PI3K inhibitor such as a compound of Formula I or a pharmaceutically acceptable salt thereof and at least one HDAC inhibitor of Formula II or a pharmaceutically acceptable salt thereof.

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Photocatalytic pilot scale degradation study of pyrimethanil and of its main degradation products in waters by means of solid-phase extraction followed by gas and liquid chromatography with mass spectrometry detection

Aqueous solutions of Pyrimethanil, as technical grade product (TP), with 98.2% purity, and commercial formulation (CF), containing 40% (w/v) of Pyrimethanil, were submitted to photocatalytic degradation under sunlight in the presence of TiO2 as catalyst in a preindustrial pilot plant. Complete Pyrimethanil degradation was achieved after ca. 230 min of irradiation, in both TP and CF, but total mineralization was not observed, as was demonstrated by the TOC values of 3-4 mg/L, measured at the end of the experiments (907 min). A qualitative and quantitative study of the degradation products (DPs) generated during the process was performed by GC- MS, using El and Cl as ionization modes, and by LC-API-MS, using Atmospheric Pressure Chemical Ionization (APCI) and Electrospray (ES) interfacing techniques. Up to 22 compounds could be detected as degradation intermediates. To evaluate the extraction efficiency of these DPs from the aqueous solution, specially for the more polar intermediates, a recovery study was performed with Pyrimethanil and seven of the commercially available DPs. Liquid-liquid extraction (LLE) and solid-phase extraction (SPE), with different sorbents, were compared. A SPE method using Lichrolut-EN cartridges was selected as the most adequate, but recoveries ?60% were obtained for four of the DPs studied (aniline formamide, 1,3-benzenediol, and 4,6- dimethyl-2-pyrimidinamine). Structure identification of DPs allowed us to propose two main routes in the degradation process. One route involves the attack of hydroxyl radicals to the pyrimidine and benzene rings with further rings opening and the other one corresponds to a photoinduced hydrolysis of the molecule by the amine group bonds. Aqueous solutions of Pyrimethanil, as technical grade product (TP), with 98.2% purity, and commercial formulation (CF), containing 40% (w/v) of Pyrimethanil, were submitted to photocatalytic degradation under sunlight in the presence of TiO2 as catalyst in a preindustrial pilot plant. Complete Pyrimethanil degradation was achieved after ca. 230 min of irradiation, in both TP and CF, but total mineralization was not observed, as was demonstrated by the TOC values of 3-4 mg/L, measured at the end of the experiments (907 min). A qualitative and quantitative study of the degradation products (DPs) generated during the process was performed by GC-MS, using El and Cl as ionization modes, and by LC-API-MS, using Atmospheric Pressure Chemical Ionization (APCI) and Electrospray (ES) interfacing techniques. Up to 22 compounds could be detected as degradation intermediates. To evaluate the extraction efficiency of these DPs from the aqueous solution, specially for the more polar intermediates, a recovery study was performed with Pyrimethanil and seven of the commercially available DPs. Liquid-liquid extraction (LLE) and solid-phase extraction (SPE), with different sorbents, were compared. A SPE method using Lichrolut-EN cartridges was selected as the most adequate, but recoveries ? 60% were obtained for four of the DPs studied (aniline, formamide, 1,3-benzenediol, and 4,6-dimethyl-2-pyrimidinamine). Structure identification of DPs allowed us to propose two main routes in the degradation process. One route involves the attack of hydroxyl radicals to the pyrimidine and benzene rings with further rings opening and the other one corresponds to a photoinduced hydrolysis of the molecule by the amine group bonds.

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Fused ring compound and including the fused ring compound of the organic light-emitting device (by machine translation)

The invention provides a compound represented by the formula 1 of the fused ring compound and that including the fused ring compound of the organic light-emitting device. [Formula 1] (by machine translation)

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Poly (ethylene glycol)-bound sulphonic acid as a novel catalyst for synthesis of benzoxazoles

ABSTRACT Ahighly efficient, simple and rapid method for the preparation of various 2-aminobenzoxazoles and other benzoxazole derivatives using a catalytic amount of poly (ethylene glycol)-bound sulphonic acid (PEG-SO3H) is described. PEG-SO3H is found to be economical and reusable catalyst with low catalytic loading. The percentage yield was found to be satisfactory, experimental set-up and purification of final products is facile and easy. GRAPHICAL ABSTRACT.

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Ru/C: A simple heterogeneous catalyst for the amination of azoles under ligand free conditions

A ligand free Ru/C-catalyzed amination of 2-halo azoles with a broad scope of aminating reagents has been developed. A variety of 2-aminoazole derivatives were synthesized in moderate to good yields by utilizing this protocol. The methodology is operationally simple and not sensitive to air and moisture. It provides potentially useful products by using an inexpensive and recyclable catalytic system under ligand free conditions without significant loss of its catalytic activity up to four cycles. This journal is

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