Application of 1017779-69-9, As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 1017779-69-9 name is 3-Fluoro-4-(trifluoromethoxy)aniline, This compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below.
Example 120 6-(5,6-difluoro-2-methyl-lH-benzimidazol-l-yl)-N-[3-fluoro-4- ) To a mixture of l-(6-chloropyrazin-2-yl)-5,6-difluoro-2-methyl-lH-benzo[d]imidazole (140 mg, 0.5 mmol) in DME was added K3P04 (360 mg, 0.85 mmol), Pd2dba3 (23 mg, 0.0125 mmol) and X-Phos (24 mg, 0.025 mmol). The reaction mixture was stirred at 100 C for 4 hours, then cooled to room temperature. The product was filtered and washed with DME, then dried under reduced pressure to give the title compound as a white solid (195 mg, 92%). ]H NMR (500 MHz, DMSO-i) delta 10.37 (br. s., 1 H), 8.40 (d, 7=2.52 Hz, 2 H), 7.91 (dd, 7=13.24, 2.52 Hz, 1 H), 7.66 – 7.81 (m, 2 H), 7.52 (t, 7=8.67 Hz, 1 H), 7.44 (dt, 7=8.99, 1.34 Hz, 1 H), 2.58 – 2.70 (S, 3 H); MS m/z 440.4 (ESI) [M+H]+.
At the same time, in my other blogs, there are other synthetic methods of this type of compound, 3-Fluoro-4-(trifluoromethoxy)aniline, and friends who are interested can also refer to it.
Reference:
Patent; PTC THERAPEUTICS, INC.; BAIAZITOV, Ramil; CHOI, Soongyu; DU, Wu; HWANG, Seongwoo; LEE, Chang-Sun; LIU, Ronggang; MOON, Young-Choon; PAGET, Steven, D.; REN, Hongyu; SYDORENKO, Nadiya; WILDE, Richard, Gerald; WO2015/76800; (2015); A1;,
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