With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.24340-77-0,4-Bromoisothiazole,as a common compound, the synthetic route is as follows.
To a reaction flask were added compound 22 (100 mg, 0.195 mmol), 4-bromoisothiazole (50 mg, 0.293 mmol), Pd(dppf)Cl2 (5 mg, 0.006 mmol) and sodium carbonate (60 mg, 0.558 mmol), 5 mL glycol dimethyl ether and 0.9 mL water were added, bubbled with nitrogen gas for 10 minutes, and the reaction was heated to 100 C in microwave and reacted for half an hour. After TLC detected the reaction was complete, the reaction was concentrated, purified by silica gel column chromatography to afford 42 mg of a product, yield: 46%. LC-MS(APCI): m/z = 469.5 (M+1)+. 1H NMR (400 MHz, CDCl3) delta 8.69 (d, J = 2.4 Hz, 1H), 8.58 (d, J = 9.6 Hz, 2H), 7.94 (d, J = 2.4 Hz, 1H), 7.74 (s, 1H), 7.67 (d, J = 9.0 Hz, 2H), 7.23 (s, 1H), 5.21 (d, J = 52.0 Hz, 1H), 3.56 (d, J = 3.1 Hz, 1H), 3.52 – 3.44 (m, 2H), 3.30 (t, J = 9.7 Hz, 1H), 2.26 – 2.19 (m, 1H), 2.03 – 1.97 (m, 1H).
24340-77-0 4-Bromoisothiazole 5200358, aisothiazole compound, is more and more widely used in various.
Reference£º
Patent; Shenzhen Targetrx, Inc.; WANG, Yihan; ZHAO, Jiuyang; AL, Yixin; (51 pag.)EP3553057; (2019); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com