- Functionalization of 4,5-Dichloropyridazin-3(2H)-one
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The functionalization of 4,5-dichloropyridazin-3(2H)-one and 4,5-dichloro-2-methyl-6-nitropyridazin-3(2H)-one was reported. A mixture of 4,5-dichloropyridazin-3(2H)-one, potassium nitrate and conc-sulfuric acid was stirred for 5 hours at 110-120°C. After cooling to room temperature, the solution was slowly poured into ice-water. The resulting yellow crystals was filtered, washed with water and dried in air to give the product. A mixture of 4,5-dichloro-6- nitropyridazin-3(2H)-one and POCl3 was refluxed for 24 hours. After cooling to room temperature, the solution was evaporated under reduced pressure. The resulting residue was slowly poured into ice-water (300 mL). Chlorination of compound 4,5-dichloro-6- nitropyridazin-3(2H)-one with phosphorus oxychloride also gave 3,4,5-trichloro-6-nitropyridazine in 72% yield. Three proton signals were also detected at d 9.0 (1H), 8.64 (1H) and 6.20 (2H) ppm in the spectrum of 1H NMR.
- Sung, Gi Hyeon,Kim, Bo Ram,Ryu, Ki Eun,Yoon, Yong-Jin
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p. 140 - 144
(2014/04/03)
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- TRICYCLIC COMPOUNDS FOR USE AS KINASE INHIBITORS
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There is provided compounds of formula (I), wherein R1, R2, X, R3 and R4 have meanings given in the description (and which compounds are optionally substituted as indicated in the description), and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PIM family kinase, such as PIM-1, PIM-2 and/or PIM-3) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease. There is also provided combinations comprising the compounds of formula (I).
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Page/Page column 70
(2013/03/26)
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- Fused heterocyclic compounds useful as kinase modulators
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Compounds having the formula (1), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, are usefuil as kinase modulators, including MK2 modulation, wherein one of E and F is a nitrogen atom and the other of E and F is a carbon atom, Z is N or CR3, and R1, R2, R3, X and Y are as defined herein.
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Page/Page column 48
(2010/11/26)
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