Related Products of 83-10-3, These common heterocyclic compound, 83-10-3, name is 1,5-Dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxylic acid, its 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.
Step 2) N-(5-hydroxypyridin-2-yl)-2.5-dimethyl-3-oxo-l-phenyl-2.3-dihydro-lH- pyrazole-4-carboxamide [0213] A suspension of 2-amino-5-hydroxypyridine hydrochloride (500 mg, 3.41 mmol) and Et3N (0.77 mL, 5.5 mmol) in DMF (8 mL) was stirred at rt for 1 hour. At the same time, to a solution of l,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-lH-pyrazole-4- carboxylic acid (0.64 g, 2.75 mmol), EtaOmicronAlphaTau (449 mg, 3.3 mmol) and EDCI (0.63 g, 3.3 mmol) in DMF (8 mL) was added Et3 (0.77 mL, 5.5 mmol) drop wise. The mixture was stirred at rt for 1 hour, followed by the addition of the above prepared mixture. The reaction was heated at 60 C for 5 hours, then cooled to rt and diluted with water (150 mL). and adjust to pH = 6 with HC1 (1 M). The mixture was extracted with EtOAc (20 mL x 4), and the combined organic phases were washed with brine (20 mL), dried over anhydrous a2S04, and concentrated in vacuo. The residue was purified by a silica gel column chromatography (DCM/MeOH (v/v) = 10/1) to give the title compound as a pale yellow solid (699 mg, 78%). MS (ESI, pos. ion) m/z: 325.1 [M+H]+.
Statistics shows that 1,5-Dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxylic acid is playing an increasingly important role. we look forward to future research findings about 83-10-3.
Reference:
Patent; CALITOR SCIENCES, LLC; SUNSHINE LAKE PHARMA CO., LTD.; XI, Ning; WU, Yanjun; LIAO, Min; FENG, Yanming; WO2014/22116; (2014); A2;,
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