application | fexostat impurity 7 is an impurity produced in the non-buxostat synthesis process, and can also be used as a laboratory research and development process and chemical medicine synthesis process. |
Preparation | 2-[3-((hydroxyimino) methyl)-4-(2-methylpropoxy) phenyl]-4-methylthiazol-5-carboxylic acid (febuxostat impurity 7) preparation of compounds: add 2-[3-((hydroxyimino) methyl)-4-(2-methylpropoxy) phenyl]-4-methylthiazol-5-carboxylate ethyl ester (100g) methanol (500 ml) solution (22.10g, in 500 ml of water) to the pre-cooled sodium hydroxide solution. The reaction mixture was heated to 75°C and stirred at the same temperature for 30 minutes. Water (5g) was added to the reaction mixture and the reaction mixture was cooled to 25°C. Methanol (100ml) and water (100ml) were added to the reaction mixture. Use aqueous hydrochloric acid to adjust the pH to 2.0-3.0. Stir the reaction mixture for 5 hours.
filter the precipitated solid and wash with methanol and water. Dry the resulting material. Tetrahydrofuran (270ml) and carbon (2.25gms) were added to the resulting substance. The reaction mixture was stirred for 30 minutes and filtered through hyflow. The solvent is completely distilled from the filtrate. Methanol (450ml) was added to the resulting compound and stirred at 60°C for 30 minutes. The reaction mixture was cooled to 25°C and stirred for 2 hours. Filter the precipitated solid and dry the substance to obtain the pure title compound febuxostat impurity 7. Output: 70g. |
biological activity | Febuxostat impurity 7 is Febuxostat impurity. Febuxostat is a selective xanthine oxidase (XO) inhibitor with Ki of 0.6 nM. |