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We reveal here a direct autoxidative phosphorylation of heteroarenes induced by oxygen under metal-free and solvent-free conditions. This new methodology provides an economical, operationally simple, and environmentally friendly approach toward (Het)C(sp2)-P formation with medium to excellent yields. Heteroarenes including thiazole and quinoxaline derivatives are applicable under standard conditions, which is testified via a radical mechanism.

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The preclinical characterization of novel octahydropyrrolo[3,4-c]pyrroles that are potent and selective orexin-2 antagonists is described. Optimization of physicochemical and DMPK properties led to the discovery of compounds with tissue distribution and duration of action suitable for evaluation in the treatment of primary insomnia. These selective orexin-2 antagonists are proven to promote sleep in rats, and this work ultimately led to the identification of a compound that progressed into human clinical trials for the treatment of primary insomnia. The synthesis, SAR, and optimization of the pharmacokinetic properties of this series of compounds as well as the identification of the clinical candidate, JNJ-42847922 (34), are described herein.

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The synthesis of some quinoxalinesulfonyl derivatives is described. Two of the synthesized derivatives, 2-oxo-1,2-dihydroquinoxaline-6-sulfonyl azide (3a) and 2,3-dioxo-1,2,3,4-tetrahydroquinoxaline-6-sulfonyl azide (3b), were screened in vitro for their growth inhibitory activity against nine strains of Gram-positive and seven strains of Gram-negative bacteria, along with two fungal isolates. The two compounds showed broad spectrum (in vitro) activity against the bacterial strains. Copyright Taylor & Francis Inc.

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The invention discloses a quinoxaline-containing 1, 4 – pentadiene – 3 – ketone derivative, characterized in that the general formula as follows: Wherein R1 Is phenyl, substituted phenyl or substituted aryl heterocyclic group; R2 In order to of the quinoxaline structure 5, 6, 7 or 8 bit contained on one or more of the hydrogen atom, methoxy, nitro, methyl, trifluoromethyl or halogen atom. The compounds of the invention to tobacco mosaic virus (TMV) has higher treatment, protection and deactivating, demonstrates higher antiviral activity, can be used for the preparation of plant virus pesticide. (by machine translation)

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This invention relates to herbicidal quinoxalinyloxy ethers, herbicidal compositions containing said ethers, and methods of using said compounds as herbicides.

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As part of our program aimed at the development of potent excitatory amino acid antagonists, we synthesized and evaluated a series of substituted 1,2,4- triazolo[4,3-a]quinoxalin-4(5H)-ones, 4, tetrazolo[1,5-a]quinoxalin-4(5H)- ones, 5, and pyrazolo[1,5-c]quinazolin-5(6H)-ones, 6, and an imidazo[1,2- a]quinoxalin-4(5H)-one, 7. In general, the same heterocycles which demonstrated the best affinity for the AMPA receptor also demonstrated the best affinity for the glycine site on the NMDA receptor complex. 1-Propyl- 7,8-dichloro-1,2,4-triazolo[4,3-a]quinoxalin-4(5H)-one, 4d, was found to bind with the greatest affinity to the AMPA receptor with an IC50 of 0.83 muM and antagonized 40 muM AMPA-induced depolarization in the cortical slice preparation with an IC50 of 44 muM. 7,8-Dichloro-1,2,4-triazolo[4,3- a]quinoxalin-4(5H)-one, 4a, and 7,8-dichloroimidazo[1,2-a]quinoxalin-4(5H)- one, 7, possessed the best affinity for the glycine site with IC50 values of 0.63 and 1.26 muM, respectively. It is noteworthy that the SAR for the heterocyclic compounds did not directly parallel that of known quinoxalinediones (e.g. DNQX, 2, and DCQX, 15) at the AMPA receptor nor that of the kynurenic acids at the glycine site on the NMDA receptor complex.

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The synthesis of new 2-fluoro-, 3-fluoro- and 2,3-difluoroquinoxalines by nucleophilic substitution with cesium fluoride as coupled with 18-crown-6 and their herbicidal activities are described.

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Colors to dye for: Palladium-catalyzed regiospecific N-heteroarylations of amidines with 2-halo-N-heteroarenes leads to a structurally diverse library of BF2/amidine-based complexes. These dyes not only present full-visible-color solid-state emissions with large Stokes shifts and high fluorescence quantum yields, but also exhibit a full-color-tunable mechanofluorochromic nature. Copyright

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The oxidative magnesiation of nitrogen-containing pi-deficient halogenoheteroaromatics using active magnesium was accomplished. Both magnesiation followed by addition of a carbonyl compound (Grignard reaction) and magnesiation in the presence of a carbonyl compound (Barbier reaction) were carried out to afford the corresponding product. Especially, the latter method enabled fused halogenodiazines such as 4-chloro-1-phenyl-1H-pyrazolo[3,4-d]pyrimidine or 2-chloroquinoxaline to magnesiate at a mild temperature (-20 to 30 C).

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The title betaines are prepared: the two triazinyl betaines undergo spontaneous thermal dimerisation, and all add a variety of 2?, 4?, and/or 6? dipolarophiles.The regio- and stereo-chemistry of the addition are elucidated and rationalised.The pyridyl adducts undergo quaternisation and ring opening to tropolones.

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