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We describe the catalytic amination of beta-(hetero)arylethyl ethers with amines using the organic superbase t-Bu-P4 to obtain beta-(hetero)arylethylamines. The reaction has a broad substrate scope and allows the transformations of electron-deficient and electron-neutral beta-(hetero)arylethyl ethers with various amines including pyrrole, N-alkylaniline, diphenylamine, aniline, indole, and indoline derivatives. Mechanistic studies indicate a two-reaction pathway of MeOH elimination from the substrate to form a (hetero)arylalkene followed by the hydroamination of the alkene.

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A highly enantioselective rhodium-catalyzed arylation of benzoxazinones and quinoxalinones with arylboroxines was realized for the first time by employing a simple sulfur-olefin as the ligand. This protocol provides an efficient access to chiral 3,4-dihydrobenzo[1,4]oxazin-2-ones and dihydroquinoxalinones with exceptionally high enantiomeric purity (up to 99.9% ee).

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 35857-89-7, name is 6-Chloropyridazine-3-carbonitrile, introducing its new discovery. Recommanded Product: 6-Chloropyridazine-3-carbonitrile

The present invention provides compounds having excellent 11-HSD1 inhibitory activity. A compound represented by the following formula (I): [wherein X 1 represents an oxygen atom, or the formula -(CR 11 R 12 ) p -, etc., Y 1 represents a hydrogen atom, a hydroxyl group, etc., Z 1 represents an oxygen atom or the formula -(NR 14 )-, R 1 represents a hydrogen atom, a halogen atom, a cyano group, a C 1-4 alkyl group, a C 1-4 alkyl group substituted with 1 to 3 halogen atoms, a C 1-4 alkoxy group, a C 1-4 alkoxycarbonyl group, a carboxyl group, a carbamoyl group, or an amino group, and m represents an integer of 1 or 2, and R 2 represents a hydrogen atom or a C 1-4 alkyl group, and n represents an integer of 1 or 2]

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Pyridazine – Wikipedia,
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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 35857-89-7, name is 6-Chloropyridazine-3-carbonitrile, introducing its new discovery. HPLC of Formula: C5H2ClN3

The invention discloses a bromo two fluorine ethyl acetate as a acylation reagent prepared N – aryl formamide, to N – alkyl amine as the raw material, bromo two fluorine ethyl acetate as a acylating agent, copper as a catalyst, by adding different ligand, alkali and the like, in a solvent in the reaction, for 100 – 120 C lower, stirring for 10 – 14 hours; the end of the reaction, the reaction solution is filtered, the filtrate obtained; to the filtrate to concentrate and the Rotavapor for removing the solvent the residue obtained, through the silica gel column chromatography of the residue, and by the eluant for executing leaching, according to the actual gradient of collecting the effluent; combining contains product effluent, towards the combined effluent concentrate to solvent, finally through drying under vacuum to obtain the target product. Raw materials of the invention is simple and easy, simple preparation process, less pollution, low energy consumption, advantage of high productive rate. (by machine translation)

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Pyridazine – Wikipedia,
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Synthesis of three clinical candidates for medicines, a human urate transporter-1 inhibitor, an arginine vasopressin antagonist, and a 17beta-hydroxysteroid dehydrogenase type-3 inhibitor, is described. These compounds were synthesized via construction of their 3,4-dihydro-2H-benzo[b][1, 4]oxazine, dibenzodiazepine, and dibenzazocine skeletons, respectively, using the reductive ring-expansion reaction of the corresponding bicyclic or tricyclic oximes with diisobutylaluminum hydride.

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Pyridazine – Wikipedia,
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The benzoxazinone and dihydroquinoxalinone fragments were employed as novel acetyl lysine mimics in the development of CREBBP bromodomain ligands. While the benzoxazinone series showed low affinity for the CREBBP bromodomain, expansion of the dihydroquinoxalinone series resulted in the first potent inhibitors of a bromodomain outside the BET family. Structural and computational studies reveal that an internal hydrogen bond stabilizes the protein-bound conformation of the dihydroquinoxalinone series. The side chain of this series binds in an induced-fit pocket forming a cation-pi interaction with R1173 of CREBBP. The most potent compound inhibits binding of CREBBP to chromatin in U2OS cells.

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Pyridazine – Wikipedia,
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Benzo[de]isoquinoline-1,3-dione of Formula or a pharmaceutically acceptable salt thereof wherein R is hydrogen or a protecting group typically used in the art for protecting alcohols and R1-R5 are each independently chosen from H, Cl, Br, F, straight or branched alkyl C1-C8 alkyl, C3-C8 cycloalkyl, heterocycle or bridged heterocycle of 4-9 atoms containing 1-3 heteroatoms, ?(CR?2)nOR6, ?(CR?2)nN(R6)2, ?(CR?2)nNR6COR7, ?(CR?2)nNR6SO2OR7, ?(CR?2)nNR6SO2 N(R6)2, ?(CR?2)nOSO2 N(R6)2, ?(CR?2)nCN, ?(CR?2)n(NOR6)R7, NO2, CF3, ?(CR?2)nSOmR7, ?(CR?2)nSOmR7, ?(CR?2)nCO2R6, ?(CR?2)nCON(R6)2, Ph, and any two of R1-R5 may form a substituted or unsubstituted ring of 5-7 total atoms having 0-2 heteroatoms are claimed which are selective inhibitors of bacterial DNA gyrase and DNA topoisomerase useful in antibacterial agents. Methods for their preparation and formulation as well as novel intermediates useful in the preparation of the final products are also claimed.

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Pyridazine – Wikipedia,
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Carvedilol is a uniquely effective drug for the treatment of cardiac arrhythmias in patients with heart failure. This activity is in part because of its ability to inhibit store-overload-induced calcium release (SOICR) through the RyR2 channel. We describe the synthesis, characterization, and bioassay of ca. 100 compounds based on the carvedilol motif to identify features that correlate with and optimize SOICR inhibition. A single-cell bioassay was employed on the basis of the RyR2-R4496C mutant HEK-293 cell line in which calcium release from the endoplasmic reticulum through the defective channel was measured. IC50 values for SOICR inhibition were thus obtained. The compounds investigated contained modifications to the three principal subunits of carvedilol, including the carbazole and catechol moieties, as well as the linker chain containing the beta-amino alcohol functionality. The SAR results indicate that significant alterations are tolerated in each of the three subunits.

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Pyridazine – Wikipedia,
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We report the synthesis and structure-activity relationships of a class of tetracyclic butyrophenones that exhibit potent binding affinities to serotonin 5-HT2A and dopamine D2 receptors. This work has led to the discovery of 4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H- pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl) -1-(4-fluorophenyl)-butan-1-one 4-methylbenzenesulfonate (ITI-007), which is a potent 5-HT2A antagonist, postsynaptic D2 antagonist, and inhibitor of serotonin transporter. This multifunctional drug candidate is orally bioavailable and exhibits good antipsychotic efficacy in vivo. Currently, this investigational new drug is under clinical development for the treatment of neuropsychiatric and neurological disorders.

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Pyridazine – Wikipedia,
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The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 35857-89-7 is helpful to your research. Related Products of 35857-89-7

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The synthesis of benzoxazinyl-pyridazinone compounds is described. The novel compounds are cardiotonic agents and inhibitors of phosphodiesterase fraction III. In addition, the compounds are useful as smooth muscle relaxants and bronchodilators

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