Category: 14521-81-4

Reference of 14521-81-4, The chemical industry reduces the impact on the environment during synthesis 14521-81-4, name is 3-Fluoro-1H-pyrazole, I believe this compound will play a more active role in future production and life.

A mixture of (5)-S -chloro-N-( 1 -cyclopropyl-2,2,2-trifluoroethyl)-7-methylpyrazolo[ 1,5 -aj pyrimidine-3 -carboxamide (70 mg, 0.21 mmol), 3-fluoro- 1H-pyrazole(18 mg, 0.21 mmol), and K2C03 (58 mg, 0.42 mmol) in DMF (2 mL) was stirred at 60 C for 2 h, poured into H20 (10 mL), and extracted with EA (30 mL x 3). The combined organic phases were washed with H20 (50 mL) and brine (50 mL), dried over anhydrous Na2SO4 and filtered. The filtrate was concentrated in vacuo, and the residue was purified by silica gel columnchromatography (PE/EA = 2/1) and preparative HPLC (10 mM NH4HCO3/MeCN) to afford thetitle compound (14 mg, 24%) as a white solid. ?H NMR (400 MHz, MeOD-d4): 5 8.59 (s, 1H),8.55 (t, J= 2.4 Hz, 1H), 7.65 (s, 1H), 7.44 (q, J= 2.8 Hz, 1H), 4.36-4.30 (m, 1H), 2.92 (s, 3H),1.40-1.34 (m, 1H), 0. 82-0.75 (m, 1H), 0.70-0.58 (m, 2H), 0.52-0.46 (m, 1H). LC-MS m/z:383.1 [M+Hj. HPLC: Purity (214 nm): 93%; tR= 8.83 min.

In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles, 3-Fluoro-1H-pyrazole, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; LYSOSOMAL THERAPEUTICS INC.; SKERLJ, Renato, T.; BOURQUE, Elyse Marie Josee; LANSBURY, Peter, T.; GOOD, Andrew, C.; (391 pag.)WO2017/176960; (2017); A1;,
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Some common heterocyclic compound, 14521-81-4, name is 3-Fluoro-1H-pyrazole, molecular formula is C3H3FN2, 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. category: pyrazoles-derivatives

(5)-N-(4-Cyano-3-(trifluoromethyl)phenyl)-3-(3-fluoro-lH-pyrazol- l-yl)-2-hydroxy-2- methylpropanamide Ci5Hi2F4N402 (1012) (0755) (0756) [00344] To a solution of 3-fluoro-pyrazole (0.20 g, 0.00232 mol) in anhydrous THF (10 mL), which was cooled in an ice water bath under an argon atmosphere, was added sodium hydride (60% dispersion in oil, 0.24 g, 0.00582 mol). After addition, the resulting mixture was stirred for 3 h. (7?)- 3-Bromo-N-(4-cyano-3-(trifluoromethyl)phenyl)-2-hydroxy-2-methylpropanamide (8, 0.82 g, 0.00232 mol) was added to above solution, and the resulting reaction mixture was allowed to stir overnight at RT under argon. The reaction was quenched by water, and extracted with ethyl acetate. The organic layer was washed with brine, dried with MgS04, filtered, and concentrated under vacuum. The product was purified by a silica gel column using ethyl acetate and hexanes (2: 1) as eluent to afford 0.36 g of the compound as white needles. (0757) [00345] Compound 1012 was characterized as follows: lH NMR (400 MHz, DMSO-i delta 10.39 (s, 1H, NH), 8.47 (d, = 2.0 Hz, 1H, ArH), 8.24 (dd, = 8.8 Hz, = 2.0 Hz, 1H, ArH), 8.11 (d, = 8.8 Hz, 1H, ArH), 7.55 (t, J = 3.0 Hz, 1H, Pyrazole-H), 6.29 (s, 1H, OH), 5.93-5.91 (m, 1H, Pyrazole- H), 4.34 (d, = 13.6 Hz, 1H, CH), 4.15 (d, = 13.6 Hz, 1H, CH), 1.36 (s, 3H, CH3); Mass (ESI, Positive): 357.0966 [M+H]+.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 14521-81-4, its application will become more common.

Reference:
Patent; UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION; NARAYANAN, Ramesh; MILLER, Duane; PONNUSAMY, Thamarai; HWANG, Dong-Jin; HE, Yali; (234 pag.)WO2017/214634; (2017); A1;,
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Reference of 14521-81-4, Each compound has different characteristics, and only by selecting the characteristics of the compound suitable for a specific situation can the compound be applied on a large scale. 14521-81-4, name is 3-Fluoro-1H-pyrazole, This compound has unique chemical properties. The synthetic route is as follows.

To a stirred solution of 4, 6-dichloro-N-(4, 4-difluorocyclohexyl) pyrimidin-2-amine (1 g, 3.54 mmol) in acetonitrile (10 mL) was added 3-fluoro pyrazole (0.36 g, 4.25 mmol) and cesium carbonate (2.30 g, 7.089 mmol). The reaction mixture was heated at 80 C for 8h. The reaction mixture was filtered and the filtrate was concentrated to afford crude product and which was purified by column chromatography (60-120 mesh) using 22% ethyl acetate in pet ether as solvent to afford 4, 6-dichloro-N-(4, 4- difluorocyclohexyl) pyrimidin-2-amine [Bj as an off-white solid (4 g, 32%). MS (M, M+2)=282.0, 284.1.

The chemical industry reduces the impact on the environment during synthesis 3-Fluoro-1H-pyrazole. I believe this compound will play a more active role in future production and life.