With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5198-88-9,2-Bromothiazole-4-carboxylic acid,as a common compound, the synthetic route is as follows.,5198-88-9
Compound 134 (0.96 g, 3.85 mmol) was dried in the tared reaction flask and weighed. This was dissolved in 30 mL dichloromethane, and 10 mL dimethylformamide was added along with a magnetic stir bar. 2-Bromothiazole-4-carboxylic acid (800.6 mg, 3.85 mmol) was weighed out and added. Diisopropylethylamine (1.0 mL, 5.7 mmol) was added followed by HATU (1.901 g, 5.00 mmol) and the reaction was stirred at room temperature overnight. This was concentrated directly onto silica and purified by column chromatography. Concentrating, then drying the pure fractions on high vacuum afforded 1.158 g of the title compound 136 (69% yield). 1H NMR (300 MHz, DMSO-d6) delta 12.14 (s, 1H), 8.57- 8.48 (m, 2H), 8.44 (s, 1H), 7.91 (ddd, J = 11.5, 8.4, 1.3 Hz, 1H), 7.52 (ddd, J = 8.4, 4.6, 3.8 Hz, 1H), 5.34 (d, J = 6.9 Hz, 1H), 4.52 (tt, J = 9.1, 7.3 Hz, 1H), 4.05 – 3.91 (m, 1H), 2.86- 2.72 (m, 2H), 2.39 (qd, J = 8.6, 2.8 Hz, 2H). m/z = 438/440 (M+H)+ (bromine isotopes).
As the paragraph descriping shows that 5198-88-9 is playing an increasingly important role.
Reference£º
Patent; RIGEL PHARMACEUTICALS, INC.; KELLEY, Ryan; LI, Hui; HECKRODT, Thilo; CHEN, Yan; MCMURTRIE, Darren; TSO, Kin; TAYLOR, Vanessa; SINGH, Rajinder; YEN, Rose; MAUNG, Jack; (256 pag.)WO2016/172560; (2016); A1;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica