With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.777-12-8,6-(Trifluoromethyl)benzo[d]thiazol-2-amine,as a common compound, the synthetic route is as follows.
777-12-8, To a stirred solution of methyl 5-chloro-2-methoxy-3-((methoxymethoxy)methyl)benzoate (122mg, 0.445mmo1) in MeOH (5m1) was added 2.2 ml iN KOH solution. The resulting mixture was stirred at 60¡ãC overnight. After cooled to rt, the reaction was partitioned between EA and 2percent citric acid. The EA layer was washed with brine, dried over Na2504 and concentrated in vacuo. To this residue was added HBTU (98mg, 0.258mmo1), DMF (3m) and DIPEA (187u, 1.075 mmo). The mixture was stirred for lOmins and then 6-(trifluoromethy)benzo[d]thiazo-2-amine (47mg, 0.2l5mmo) was added. The resuting reaction was heated at 120 ¡ãC for 24hs. After cooed to rt, the mixture was separated between EA and water. The organic ayer was washed with brine, dried over Na2SO4 and concentrated in vacuo. Purification by coumn chromatography gave the 5- choro-2-hydroxy-3 -((methoxymethoxy)methy)-N-(6-(trifluoromethy)benzo[d]thiazo -2y)benzamide as a yeow soid (37mg, 39percent). ?H NMR (400 MHz, Choroform-d) 8.16 (s, 1H), 7.99 (d, J = 2.5 Hz, 1H), 7.91 (d, J = 6.1 Hz, 1H), 7.72 (d, J = 6.1 Hz, 1H), 7.48 (d, J =2.5 Hz, 1H), 4.80 (s, 2H), 4.78 (s, 2H), 3.47 (s, 3H). MS (ESI) [M+Na] requires m/z 469.02, found m/z 468.55.
777-12-8 6-(Trifluoromethyl)benzo[d]thiazol-2-amine 2735955, athiazole compound, is more and more widely used in various fields.
Reference£º
Patent; JIN, Shengkan; AUGERI, David J.; CAO, Bin; TAO, Hanlin; (126 pag.)WO2017/201313; (2017); A1;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica