With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4576-90-3,Isothiazole-3-carboxylic acid,as a common compound, the synthetic route is as follows.
To a slurry of isothiazole-3-carboxylic acid (5.0 g, 38.7 mmol) in tert-butanol (194 mL) was added triethylamine (4.3 g, 42.6 mmol) followed by diphenyl phosphoryl azide (11.9 g, 43.3 mmol). The reaction mixture was heated to reflux for 9 h. After cooling the ambient temperature, the reaction mixture was concentrated in vacuo and the residue dissolved in ethyl acetate (300 mL). The organic layer was washed with water (100 mL), 1 N sodium hydroxide solution (50 mL), water (100 mL), brine (50 mL), and dried over anhydrous magnesium sulfate. Filtration and concentration of the filtrate in vacuo afforded a residue. Purification of the residue by column chromatography, eluting with a gradient of 0 to 10% of ethyl acetate in heptane, provided the title compound as a colorless solid (6.16 g, 79% yield): 1H NMR (300 MHz, CDCl3) delta9.03-8.98 (m, 1H), 8.58 (d, J=4.9 Hz, 1H), 7.70 (d, J=4.9 Hz, 1H), 1.53 (d, J=0.7 Hz, 9H).
4576-90-3, The synthetic route of 4576-90-3 has been constantly updated, and we look forward to future research findings.
Reference£º
Patent; Xenon Pharmaceuticals Inc.; Andrez, Jean-Christophe; Bogucki, David Earl; Burford, Kristen Nicole; Chowdhury, Sultan; Cohen, Charles Jay; Decker, Shannon Marie; Dehnhardt, Christoph Martin; Devita, Robert Joseph; Empfield, James Roy; Focken, Thilo; Grimwood, Michael Edward; Hasan, Syed Abid; Jia, Qi; Johnson, JR., James Philip; Wilson, Michael Scott; Zenova, Alla Yurevna; (287 pag.)US2018/162868; (2018); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com