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Organic chemistry; Theoretical chemistry; -carboline; QSAR; biological activity; chemical reaction path; bathochromic; electronic shift; VCD. In this methodological work, the structural activity analysis have been carried out on beta-Carboline to study the anti cancer activity and the way of improving the biological activity. The molecular spectroscopic tools were used to evaluate all the experimental data like spectral results and data were validated by the computational, HyperChem and Osiris tools. The structural, biological and physico-chemical related analyses have been performed to interpret the properties. The GPCR ligand calculated to be 0.11 for generating pharmacokinetic process, Specified drug information for the compound, was congregated from all types of structural activity which was drawn by spectral and HyperChem data. The sigma and pi interaction band gap (6.18 eV) ensured the drug consistency. The Mulliken charge process distribution was mapped, the charge orientation assignment was checked; the acquired negative charge potential consignment for the cause of antibiotic impact was verified. The molecular orbital interaction study was carried out to identify the origination of degeneracy of interaction causing drug mechanism. Using NMR spectral pattern, the chemical reaction path was recognized and the nodal region dislocation was distinguished on chemical shift. The Electronegativity (chi) and Electrophilicity charge transfer found to be 3.83 and 0.215, confirmed charge complex transfer for activating drug process in the compound. The molecular nonbonding section was thoroughly observed in order to find the occupancy energy, was the key process to initiate drug activity. The bathochromic electronic shift was observed and the existence of CT complex was discussed. The hindering of toxicity was inspected on inevitable chirality of the compound by specifying VCD spectrum.

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Optically active allylic sulphides 10-13, bearing two different leaving groups, react with organocopper reagents by selective substitution of the heterocyclic moiety leading to optically active homoallylic pivalates with chemo-, regio- and enantio-control.This selectivity seems to be related to the coordination exerted by the heterocyclic nucleus towards the organometal.

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The present invention is to provide a process for preparing a synthetic intermediate of biotin which is industrially advantageous, and discloses a process for preparing a compound represented by the formula (I) :???wherein R1 and R2 may be the same or different from each other, and each represents hydrogen atom, a benzyl group which may have a substituent(s) on the benzene ring, a benzhydryl group which may have a substituent(s) on the benzen ring, or a trityl group which may have a substituent(s) on the benzene ring, R3 represents cyano group, carboxyl group, an alkoxycarbonyl group, an alkylthiocarbonyl group, or a carbamoyl group which may have a substituent, or a salt thereof which comprises subjecting a compound represented by the formula (II-a) :???wherein the symbols have the same meanings as defined above, or a salt thereof to ring transformation.

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The present invention relates to compounds of the formula (I), or pharmaceutically acceptable salts, enantiomer or diastereomer thereof, wherein R1 to R4 and Q are as described above. The compounds may be useful for the treatment or prophylaxis of hepatitis B virus infection.

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We report a novel methodology for preparing enantiomerically pure beta-lactams, starting from nitriles in diastereomeric ratios up to 10:1. The power of the methodology was demonstrated by the efficient synthesis of the cholesterol absorption inhibitor SCH 48462.

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2,4-Disubstituted quinolines with additional substituents in positions 5-8 have been found to have anthelmintic properties. A number of 2,4-dimethoxy-6- or 8-arylquinolines have potent activity against the sheep nematode Haemonchus contortus, with LD99 values of the same order of magnitude as levamisole. These arylquinolines maintain their activity against levamisole-, ivermectin- and thiabendazole-resistant strains of H. contortus.

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Diastereocontrolled aldol-type reactions between tin(II) enolates of 3-acetyl-4(S)-ETT (6a) and 3-acetyl-4(S)-IPTT (6b) and alpha,beta-unsaturated aldehydes 7a-c were successfully carried out to give, with highly diastereoselectivity, compounds 9a-e (major products) and 10a-e (minor products).The reaction conditions were also investigated in detail.

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What is described are BET protein-inhibitory, in particular BRD4-inhibitory 2,3-benzodiazepines of the general formula (I) in which R1a, R1b, R1c, R2, R3, R4, R5, A and X have the meanings given in the description, intermediates for preparing the compounds according to the invention, pharmaceutical compositions comprising the compounds according to the invention and their prophylactic and therapeutic use for hyperproliferative disorders, in particular for tumour disorders. Also described is the use of BET protein inhibitors for benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, for neurodegenerative disorders, for inflammatory disorders, for atherosclerotic disorders and for the control of male fertility.

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Room temperature biacetyl phosphorescence enhanced via molecular organization is observed for many aromatic compounds.Micelles composed of sodium dodecyl sulfate(SDS) and hosts such as beta-cyclodextrin(beta-CD) are used to enhance the energy transfer reaction by organizing the reactants in close proximity to one another.The triplet-triplet energy transfer of several polynuclear aromatics, nitrogen heterocyclics, and heavy-atom-substituted species to biacetyl was evaluated.Both SDS and beta-CD were found to provide a superior medium for production of sensitized biacetylphosphorescence than found with homogenous solution.Typically,limits of detection of 1x 10-8 to 10-9 M in SDS and 1 x 10-7 M in beta-CD were obtained.The sensitivities of the methods are dependent on the solubility of the donor in SDS, the ability of the donor to fit into the beta-cyclodextrin cavity, and the background signal produced by the biacetyl blank solution.

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The invention discloses a quinoline substituted indole compound, containing the quinoline substituted indole compound of the pharmaceutical composition and its preparation method, also discloses quinoline substituted indole compound, containing the quinoline substituted indole compound of a pharmaceutical composition for pharmaceutical use, in particular in the preparation of medicament for treating tumor application, and preparation by inhibiting microtubule protein activity to treat other diseases or disorders of the application of the medicament. (by machine translation)

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