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Regioselective Synthesis of 3-Aminoimidazo[1,2- a ]pyrimidines with Triflic Anhydride

The regioselective synthesis of 3-aminoimidazo[1,2- a ]pyrimidines via triflic anhydride mediated amide activation and intramolecular cyclisation is reported. The nature of the added pyridine base allows access to both regioisomers from a simple common precursor. The method tolerates a range of functional groups and provides access to novel heterocyclic scaffolds.

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Brief introduction of 3-Chloro-6-methylpyridazine

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3-(3-PYRIMIDIN-2-YLBENZYL)-1,2,4-TRIAZOLO[4,3-B]PYRIDAZINE DERIVATIVES AS MET KINASE INHIBITORS

Compounds of the formula (I), in which R1, R2, R3, R3?, R4 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumours.

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Hydrazination of Pyridazines and Phthalazines

It is shown by 15N-labelling techniques that hydrazination of pyridazines partly occurs according to a reaction pathway, involving addition of the nucleophile (hydrazine), ring opening and ring closure (SN(ANRORC)-mechanism).It is also proved that phthalazines undergo hydrazination without ring opening (SN(AE)-mechanism).

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1H, 13C, and 15N NMR spectra of some pyridazine derivatives

1H, 13C, and 15N NMR chemical shifts for pyridazines 4-22 were measured using 1D and 2D NMR spectroscopic methods including 1H-1H gDQCOSY,1H-13C gHMQC,1H-13C gHMBC,and1H-15N CIGAR-HMBC experiments. (0 2010 John Wiley & Sons, Ltd.

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ANTIVIRAL AGENT

The present invention provides an integrase inhibitor. The inventors have have found the following compound of formula (I) possessing an integrase inhibitory activity. (wherein, R C and R D taken together with the neighboring carbon atoms form a ring which may be a condensed ring, Y is hydroxy, mercapto or amino; Z is O, S or NH ; R A is a group shown by (wherein, C ring is N-containing aromatic heterocycle) or the like)

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3,4,N-trisubstituted-4,5-dihydro-1H-pyrazole-1-carboxamides and their use as insecticides

3,4,N-triaryl-4,5-dihydro-1H-pyrazole-1-carboxamide compounds having an aryl moiety in the 4-position that is an optionally substituted pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or quinolinyl moiety and aryl moieties in the 3-position and the N-position that are optionally substituted phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or quinolinyl moieties, such as N-(4-chlorophenyl)-4,5- -dihydro-3-(4-fluorophenyl)-4-(5-trifluoromethyl-2- -pyridinyl)-1H-pyrazole-1-carboxamide, were prepared and found to possess insecticidal utility. 1,2-Diarylethanone compounds were converted to 1,2-diaryl-2-propen-1-one compounds by treatment with bis(dimethylamino)methane, the 1,2-diaryl-2-propen-1-one compounds were converted to 3,4-diaryl-4,5-dihydro-1H-pyrazole compounds by treatment with hydrazine, and the 3,4-diaryl-4,5-dihydro-1H-pyrazole compounds were converted to the insecticidal subject compounds by treatment with an aryl isocyanate.

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Use of N-Protected Amino Acids in the Minisci Radical Alkylation

(Equation presented) The Minisci radical alkylation has been demonstrated on a range of commercially available glycine derivatives and proceeds in good to high yield. When extending the reaction to other amino acids, competitive oxidation of the initially formed radical was overcome by using the phthalimide protecting group.

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Palladium-catalyzed cross-coupling reaction of functionalized aryl- and heteroarylbismuthanes with 2-halo(or 2-Triflyl)azines and -diazines

The palladium-catalyzed cross-coupling of highly functionalized organobismuthanes with 2-halo(or 2-triflyl)pyridines, -pyrimidines, -pyrazines, and -pyridazines is reported. The reaction tolerates numerous functional groups, including aldehydes. The synthesis of a shelf-stable (formylphenyl)bismuth reagent and its use in a cross-coupling reaction is also described. The palladium-catalyzed cross-coupling of highly functionalized organobismuthanes with 2-halo(or 2-triflyl)pyridines, -pyrimidines, -pyrazines, and -pyridazines is reported. The reaction tolerates numerous functional groups, including aldehydes. The synthesis of a shelf-stable (formylphenyl)bismuth reagent and its use in cross-coupling reactions is also described. Copyright

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Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders

To try and generate broad spectrum human rhinovirus VP1 inhibitors with more attractive physicochemical, DMPK and safety profiles, we explored the current SAR of known VP1 compounds. This lead to the identification of specific structural regions where reduction in polarity can be achieved, so guiding chemistry to analogues with significantly superior profiles to previously reported inhibitors.

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One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, HPLC of Formula: C5H5ClN2, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 1121-79-5, Name is 3-Chloro-6-methylpyridazine, molecular formula is C5H5ClN2

New iridium complexes bearing C^N=N ligand for high efficiency OLEDs

Three iridium complexes, with 3-methyl-6-(2,4-difluoro-phenyl)pyridazine (mdfppya, C^N=N type ligand) as cyclometalated ligands, and picolinate (pic) or acetylacetonate (acac) as ancillary ligand, were synthesized and structurally characterized. Among these complexes,the homoleptic one, which contains two fluorine atoms on the cyclometalated phenyl moiety to lower the LUMO and a methyl group at the cyclometalated pyridazine part to raise the HOMO, possesses the shortest emission wavelength with peak of 506 nm. Importing ancillary ligands of picolinate (pic) and acetylacetonate (acac) yielded iridium complexes with emission of longer wavelength. The investigation of photophysical, electrochemical properties, as well as quantum chemistry calculation revealed optoelectrical property differences among them, corresponding principles were discussed. Photophysical, electrochemical features, quantum chemistry simulation and electroluminescence properties were systematically investigated. All complexes were applied to organic light-emitting diodes (OLEDs) as dopant emitters and the influence of ancillary ligands on device performance is significant. Based on pic-complex, maximum device efficiencies of 41.0 cd A?1, 33.9 lm W?1 and 11.62% were achieved. Additionally, this device exhibits extremely small efficiency roll-off. The reason for this good performance is mainly attributed to the high photoluminescence quantum yield and fast radiative decay rate of the phosphor, as wells rather matched energy levels in device.

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Pyridazine – Wikipedia,
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