Electric Literature of 518057-72-2, In the chemical reaction process, reaction time, type of solvent, can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product. An updated downstream synthesis route of 518057-72-2 as follows.
To 5-amino-2-fluoro-benzamide (37 mg, 0.24 mmol) and diisopropylethylamine (124 mu, 0.71 mmol) in dichloromethane (390 mu) cooled at 0 C was added dropwise a solution of 2-fluoro-6-(4- fluorophenoxy)-3-(trifluoromethyl)benzoyl chloride (80 mg, 0.24 mmol) in dichloromethane (390 mu). The reaction was stirred at room temperature for 1 hour. The solvent was evaporated and the residue was partitioned between water and ethyl acetate. The organic phase was concentrated to dryness. The residue was dissolved in 1ml of DMSO and purified by reverse phase HPLC to afford N-(3 -carbamoyl -4-fluoro- phenyl)-2-fluoro-6-(4-fluorophenoxy)-3-(trifluoromethyl)benzamide (25.5 mg, 24%). ESI-MS m/z calc. 454.08, found 455.1 (M+l)+; retention time (Method B): 1.63 minutes (3 minute run). l NMR (400 MHz, DMSO-d6) delta 11.05 (s, 1H), 7.98 (dd, J = 6.4, 2.8 Hz, 1H), 7.89 – 7.74 (m, 3H), 7.71 (s, 1H), 7.40 – 7.25 (m, 5H), 6.79 (d, J = 8.9 Hz, 1H) ppm.
According to the analysis of related databases, 518057-72-2, the application of this compound in the production field has become more and more popular.
Reference:
Patent; VERTEX PHARMACEUTICALS INCORPORATED; AHMAD, Nadia; ANDERSON, Corey; ARUMUGAM, Vijayalaksmi; ASGIAN, Iuliana, Luci; CAMP, Joanne, Louise; FANNING, Lev Tyler, Dewey; HADIDA RUAH, Sara, Sabina; HURLEY, Dennis; SCHMIDT, Yvonne; SHAW, David; SHETH, Urvi, Jagdishbhai; THOMSON, Stephen, Andrew; (691 pag.)WO2019/14352; (2019); A1;,
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