Synthetic Route of 135900-33-3, Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps,and cheap raw materials. 135900-33-3, name is 6-(Trifluoromethoxy)pyridin-3-amine. A new synthetic method of this compound is introduced below.
[0292] Compound Int-8 (100 mg, 0.53 mmol, 1.0 eq) and 6-(trifluoromethoxy)pyridin- 3-amine (190 mg, 1.06 mmol, 2.0 eq) were dissolved in DMF (3.0 mL) and the reaction mixture was cooled down to 0 C. HATU (221 mg, 0.58 mmol, 1.1 eq) and DIPEA (136 mg, 1.06 mmol, 2.0 eq) were added to the reaction mixture at 0 C. 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. After completion of the reaction, the reaction mixture was poured into ice-cold water. The formed solid was filtered, washed and dried under vacuum to give 40 mg of the desired compound 127 as a pale-yellow solid in 21% yield. 97.88% purity as determined by HPLC at 215 nm. 1H NMR (400 MHz, DMSO-d6): delta 10.97 (s, 1H), 8.94 (dd, J = 4.4 Hz, 1.6 Hz, 1H), 8.72 (d, J = 2.4 Hz, 1H), 8.40 (dd, J = 8.8 Hz, 2.4 Hz, 1H), 8.34 (d, J = 7.6 Hz, 1H), 8.20 (s, 1H), 7.91 (s, 1H), 7.60 (dd, J = 8.4 Hz, 4.4 Hz, 1H), 7.37 (d, J = 8.8 Hz, 1H), 2.57 (s, 3H). ESI m/z =348.27 [M+H]+.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,135900-33-3, its application will become more common.
Reference:
Patent; ACTAVALON, INC.; DNEPROVSKAIA, Elena, V.; HOLZWARTH, Michael, S.; RYCHNOVSKY, Scott, D.; (184 pag.)WO2018/85348; (2018); A1;,
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