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The rate of alkaline hydrolysis of the novel compound 2-(3-nitrophenoxy)quinoxaline 1 increases with increasing head group size in a series of cationic micellized surfactants (C16H33NR3Cl and C16H33NR3OH: R = Me, Et, n-Pr and n-Bu). The reactivity increase with increasing head group size is related to the disruption of the hydration of hydroxide ion.

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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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A facile and efficient protocol for palladium-catalyzed Miyaura borylation reaction of chloropyrazines with B2pin2has been developed. A certain range of difficult-to-access pyrazine boronic esters can be easily prepared from the corresponding chloropyrazines in moderate to good yields.

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A simple and rapid method for the preparation of a series of novel quinoxaline derivatives in the presence of Ag+ is reported.

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Malononitrile could be utilized as a synthon for the carbonyl moiety via a one-pot process that was initiated via base-mediated SNAr substitution of a heteroaryl halide. Subsequent peracetic acid oxidation of the resultant anion delivered an electrophilic acyl nitrile in situ that readily reacted with added nucleophiles to afford heteroaryl carboxylic acid derivatives. The reaction of the sodium salt of malononitrile with a series of heteroaryl chlorides followed by the subsequent addition of an amine and peracetic acid provided the corresponding heteroaryl amides.

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Using Pd-catalyzed Stille cross-coupling reactions, we report here the synthesis of various mono- or bis(tri-n-butylstannyl)diazines which were reacted with various halogenated diazines to access to various polyaza heterocyclic derivatives.

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The present invention provides an organic electroluminescent compound having a structure, of Formula I suitable for use as a light emitting layer host material and a triplet state annihilation, suitable for use as a light emitting layer host material in which holes and electrons are recombined in a light emitting layer and, improve the color purity, of HOMO devices, while preventing excitons from returning back LUMO, to the transport layer while increasing the device efficiency, The present invention provides a light emitting layer host material, using, an organic electroluminescent compound as, a light emitting layer host material, and a method of fabricating the organic electroluminescent compound OLED. (by machine translation)

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Suzuki-Miyaura (SM) cross-couplings of 2-pyridyl MIDA boronates can be successfully carried out in the complete absence of copper by attenuation of the Lewis basicity associated with the pyridyl nitrogen using selected substituents (e.g., fluorine or chlorine) on the ring. This strategy imparts additional synthetic options compared with existing approaches based on the use of Lewis acids or N-oxides. Thus, access to highly valued 2-substituted pyridyl rings via an initial Suzuki-Miyaura coupling can be followed by dehalogenation, SNAr reactions, or a second SM coupling to arrive at 2,6-disubstituted pyridyl arrays, all run in a single pot, enabled by micellar catalysis in water. Accessing targets within drug-like space is demonstrated in a four-step, one-pot sequence. Computational data suggest that the major role being played by electron-withdrawing substituents in promoting these cross-couplings without the need for copper is to slow the rates of protodeboronation of intermediate 2-pyridylboronic acids.

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A new efficient procedure for the chlorination of hydroxyquinoxaline derivatives into the corresponding chlorides is described. It has been found that the use of 1-chlorobutane produces the highest yield, reduces the time of reaction and facilitates direct formation of crystals without any purification.

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Thirty compounds possessing quinoxaline structure bearing either substituted arylmethylmercapto-, arylmethylsulfinyl group or a piperazinyl moiety in position 2 were prepared in order to evaluate an antiulcer and gastroprotective activity in rat pylorus ligature, in comparison with omeprazole and ranitidine at the dose of 100 mg/kg after oral administration. Among the compounds of the first group one third showed a moderate activity being about half potent as omeprazole whereas in the second group compound 5b exhibited an activity superior to that of ranitidine accompanied with the lowest incidence of lesions and mortality and another compound (5i) was equiactive as ranitidine.

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