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.,4576-90-3
To a slurry of isothiazole-3-carboxylic acid (5.0 g, 38.7 mmol) in terf-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 hours. 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 (0805) 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): 1FI NMR (300 MHz, CDCIs) 9.03-8.98 (m, 1 H), 8.58 (d, J = 4.9 Hz, 1 H), 7.70 (d, J = 4.9 Hz, 1 H), 1.53 (d, J = 0.7 Hz, 9H).
As the paragraph descriping shows that 4576-90-3 is playing an increasingly important role.
Reference£º
Patent; XENON PHARMACEUTICALS INC.; FOCKEN, Thilo; ANDREZ, Jean-Christophe; BURFORD, Kristen Nicole; DEHNHARDT, Christoph Martin; GRIMWOOD, Michael Edward; JIA, Qi; LOFSTRAND, Verner Alexander; WILSON, Michael Scott; ZENOVA, Alla Yurevna; WESOLOWSKI, Steven Sigmund; SUN, Shaoyi; (205 pag.)WO2020/47323; (2020); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com