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The invention pertains to new pyrrolidyl derivatives of benzo-fused aza heteroaromatic compounds that serve as effective phosphodiesterase (PDE) inhibitors. The invention also relates to compounds that are selective inhibitors of PDE-IO. The invention further relates to intermediates for preparation of such compounds; pharmaceutical compositions comprising such compounds; and the use of such compounds in methods for treating certain central nervous system (CNS) or other disorders. The invention relates also to methods for treating neurodegenerative and psychiatric disorders, for example psychosis and disorders comprising deficient cognition as a symptom. Formula (I).

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Reference:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N491 | ChemSpider

 

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A newly engineered palladacycle that contains substituents on the biphenyl rings along with the ligand HandaPhos is especially well-matched to an aqueous micellar medium, enabling valued Suzuki-Miyaura couplings to be run not only in water under mild conditions, but at 300 ppm of Pd catalyst. This general methodology has been applied to several targets in the pharmaceutical area. Multiple recyclings of the aqueous reaction mixture involving both the same as well as different coupling partners is demonstrated. Low temperature microscopy (cryo-TEM) indicates the nature and size of the particles acting as nanoreactors. Importantly, given the low loadings of Pd invested per reaction, ICP-MS analyses of residual palladium in the products shows levels to be expected that are well within FDA allowable limits.

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Reference:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N703 | ChemSpider

 

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Product Details of 1448-87-9, New research progress on 1448-87-9 in 2021. Chemistry is a science major with cience and engineering. The main research directions are chemical synthesis, preparation and modification of special coatings, and research on the structure and performance of functional materials.1448-87-9, Name is 2-Chloroquinoxaline, molecular formula is C8H5ClN2. In a article,once mentioned of 1448-87-9

A newly engineered palladacycle that contains substituents on the biphenyl rings along with the ligand HandaPhos is especially well-matched to an aqueous micellar medium, enabling valued Suzuki-Miyaura couplings to be run not only in water under mild conditions, but at 300 ppm of Pd catalyst. This general methodology has been applied to several targets in the pharmaceutical area. Multiple recyclings of the aqueous reaction mixture involving both the same as well as different coupling partners is demonstrated. Low temperature microscopy (cryo-TEM) indicates the nature and size of the particles acting as nanoreactors. Importantly, given the low loadings of Pd invested per reaction, ICP-MS analyses of residual palladium in the products shows levels to be expected that are well within FDA allowable limits.

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Reference:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N703 | ChemSpider

 

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The invention discloses a fragrant nitrile or heteroaromatic nitrile compound preparation method, the method comprises the following steps: under protection of inert gas, in a solvent, in the nickel catalyst and ligand, metal zinc, and under the action of the additive, the cyano reagent with a halo aromatic hydrocarbon or the halogenating is mixed aromatic hydrocarbon reaction can be. The present invention provides a preparation method, the use of a readily available and inexpensive nickel catalyst and ligand, can be mild, efficiently realize the halogenating is mixed halo aromatic hydrocarbon or aromatic hydrocarbon can particularly will be cheap and easily obtained but the reaction low activity of the chlorinated aromatic hydrocarbon or aromatic hydrocarbon […] with toxicity is relatively small of the cyano reagent reaction, to prepare the fragrant nitrile or heteroaromatic nitrile compounds. Preparation method of this invention not only has simple operation, moderate, high efficiency and the like, but also has good functional group compatibility and universality and other characteristics of the substrate. (by machine translation)

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Quinoxaline – Wikipedia,
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A series of 3-aryl piperidine analogs with 2-piperidinoalkylamino or 2-piperidinoalkyloxy fused bicyclic rings were prepared and found to be potent and efficacious human dopamine D4 agonists. The synthesis and structure-activity relationship (SAR) studies that led to the identification of these compounds are discussed.

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Quinoxaline – Wikipedia,
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The enantioselective hydrogenation of 2-alkyl- and 2-aryl-subsituted quinoxalines and 2,3-disubstituted quinoxalines was developed by using the cationic Ru(eta6-cymene)(monosulfonylated diamine)(BArF) system in high yields with up to 99% ee. The counteranion was found to be critically important for the high enantioselectivity and/or diastereoselectivity.

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This article presents the photophysical properties of a series of diazine chromophores. The influence of five parameters has been studied: the presence of a diazine/benzodiazine fragment, the nature of the diazine fragment (1,3-diazine/1,4-diazine), the presence or not of an vinyl linker between diazine ring and phenylene fragments of the pi-conjugated bridge, the presence of a phenylene/biphenylene linker and the nature of electron donating group (dimethylamino/diphenylamino). Taguchi’s design of experiment combined with analysis of variance methodologies have been employed to highlight the main structural parameters influencing the position of absorption and emission maxima of dichloromethane solution and the extend of emission solvatochromic range exhibited by this family of chromophores.

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A novel visible-light-promoted C-P bond formation reaction in the absence of both transition metal and photoredox catalysts is disclosed. By employing easily available and inexpensive heteroaryl chlorides/bromides as substrates, a variety of heteroaryl phosphine oxides were obtained in moderate to good yields. This strategy provides a simple and efficient route to heteroaryl phosphine oxides.

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Compounds of formula 1 to formula 8 including nano-emulsion and is disclosure is organic light emitting device. Formula 1 to formula 8 to a rotating reference. (by machine translation)

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Phosphodiesterase 10A (PDE10A) inhibitors were designed and synthesized based on the dihydro-imidazobenzimidazole scaffold. Compound 5a showed moderate inhibitory activity and good permeability, but unfavorable high P-glycoprotein (P-gp) liability for brain penetration. We performed an optimization study to improve both the P-gp efflux ratio and PDE10A inhibitory activity. As a result, 6d was identified with improved P-gp liability and high PDE10A inhibitory activity. Compound 6d also showed satisfactory brain penetration, suppressed phencyclidine-induced hyperlocomotion and improved MK-801-induced working memory deficit.

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Quinoxaline – Wikipedia,
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