Reference of 4058-91-7,Some common heterocyclic compound, 4058-91-7, name is 5-Amino-1-methyl-1H-pyrazole-4-carboxylic acid, molecular formula is C5H7N3O2, 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.
To a stirred solution of Step 3 intermediate (800 mg, 5.666 mmol) in dry DMF (8 ml), 2-bromo- l-(2-chlorophenyl)ethanone (1.32 g, 5.666 mmol) was added followed by potassium fluoride (500 mg, 8.499 mmol) at room temperature and the resultant reaction mixture was stirred overnight. The mixture was quenched with water (75 mL) and ethyl acetate (30 mL). The layers were separated and the aqueous layer was extracted with ethyl acetate (3 x 100 mL). The combined organic layers were washed with water (2 x 100 mL) and dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure and the residue obtained was purified by flash silica gel column chromatography to afford 912 mg of the desired product as a solid. lH NMR (300 MHz, DMSO-d6): delta 3.54 (s, 3H), 5.31 (s, 2H), 6.31 (s, 2H), 7.43-7.53 (m, 1H), 7.55 (d, = 4.8 Hz, 1H), 7.77 (d, = 7.5 Hz, 2H), 7.95 (s, 1H).
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-1-methyl-1H-pyrazole-4-carboxylic acid, its application will become more common.
Reference:
Patent; GLENMARK PHARMACEUTICALS S.A.; KUMAR, Sukeerthi; CHAUDHARI, Sachin Sundarlal; GHARAT, Laxmikant Atmaram; KHAIRATKAR-JOSHI, Neelima; SHAH, Daisy Manish; MUKHOPADHYAY, Indranil; (327 pag.)WO2018/203298; (2018); A1;,
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