Electric Literature of 28491-52-3,Some common heterocyclic compound, 28491-52-3, name is 5-Amino-1H-pyrazol-3(2H)-one, molecular formula is C3H5N3O, traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
5-Amino-2,3-dihydro-1 H-pyrazol-3-one is dissolved in aqueous EtOH containing KOH. To this solution is added methyl 3-(3-trifluoromethyl-phenyl)-3-oxopropanoate and the mixture is stirred under reflux for 1 h 30 min. After cooling to rt, water is added and the mixture is acidified by addition of acetic acid to pH~5. The resulting precipitate is collected on a filter, washed with water and diethyl ether, and dried to give the title compound in moderate yield. Mp >;250 0C (decomp.); 1H-NMR (200 MHz, DMSO-d6), delta (ppm) 5.46 (s, 1 H); 6.05 (s, 1 H); 7.75 (t, 4 Hz, 1 H); 7.89 (d, 4 Hz, 2H); 8.07-8.12 (m, 1 H); 10.90 (br s, 1 H) and 12.25 (br s, 1 H). LC-MS m/z 296 (M+1 )
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 5-Amino-1H-pyrazol-3(2H)-one, its application will become more common.
Reference:
Patent; MERZ PHARMA GMBH &; CO. KGAA; HENRICH, Markus; BAUER, Angela; KRUeGER, Bjoern; KAUSS, Valerjans; MUeLLER, Sibylle; KUBAS, Holger; ROZHKOVS, Jevgenijs; PISKUNOVA, Irene; WO2010/139483; (2010); A1;,
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