Synthetic Route of 135900-33-3, With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.135900-33-3, name is 6-(Trifluoromethoxy)pyridin-3-amine, molecular formula is C6H5F3N2O, molecular weight is 178.11, as common compound, the synthetic route is as follows.
[0289] Quinoline-7-carboxylic acid (70 mg, 0.404 mmol, 1.0 eq) and 6- (trifluoromethoxy)-pyridin-3-amine (79 mg, 0.44 mmol, 1.1 eq) were dissolved in 1 mL of DMF and the resulting mixture was cooled down to 0 C. HATU (168 mg, 0.44 mmol, 1.1 eq) and DIPEA (0.144 mL, 0.808 mmol, 2.0 eq) were added at 0 C, and then the reaction mixture was allowed to warm up to room temperature and stirred at room temperature for 4 hrs. The progress of the reaction was monitored by LCMS and TLC. Upon completion, the reaction mixture was poured into ice-cold water. The formed solid was filtered, washed and dried in vacuo to give 20 mg of the desired compound 126 as a pale-yellow solid in 15% yield. 1H NMR (400 MHz, CDC13): delta 9.03-9.02 (dd, J = 2.8 Hz, 1.6 Hz, 1H), 8.57 (s, 1H), 8.48 (s, 1H), 8.46-8.45 (d, J = 2.8 Hz, 1H), 8.26 (s, 1H), 8.24 (brs, 1H), 8.09-8.12 (dd, J = 8.8 Hz, 1.6 Hz, 1H), 8.0-7.97 (d, J = 8.8 Hz, 1H), 7.56-7.52 (dd, J = 8.4 Hz, 4.4 Hz, 1H), 7.12-7.10 (d, J = 8.8 Hz, 1H). 99.15% purity by LCMS; m/z =334.19 [M+H]+.
Statistics shows that 135900-33-3 is playing an increasingly important role. we look forward to future research findings about 6-(Trifluoromethoxy)pyridin-3-amine.
Reference:
Patent; ACTAVALON, INC.; DNEPROVSKAIA, Elena, V.; HOLZWARTH, Michael, S.; RYCHNOVSKY, Scott, D.; (184 pag.)WO2018/85348; (2018); A1;,
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