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.105806-13-1, name is 4,6-Dichloro-5-fluoro-2-methylpyrimidine, molecular formula is C5H3Cl2FN2, molecular weight is 181, as common compound, the synthetic route is as follows.COA of Formula: C5H3Cl2FN2
[00343] To a mixture of 4,6-dichloro-5-fluoro-2-methyl-pyrimidine (390 mg, 2.15 mmol) and diisopropylethylamine (900 mu, 5.17 mmol) in dichloromethane (3.9 mL) was added l-(oxetan-3-yl)piperazine (335 mg, 2.4 mmol) . The mixture was stirred for 10 minutes. The resulting mixture was concentrated in vacuo then purified on a 40 g silica gel cartridge eluting with 0-80% ethyl acetate/heptane to provide 4-chloro- 5-fluoro-2-methyl-6-[4-(oxetan-3-yl)piperazin-l-yl]pyrirnidine (550 mg, 89%). XH NMR (400 MHz, CDC13) delta 5.35 (s, 1H), 4.92 – 4.70 (m, 2H), 4.65 – 4.41 (m, 2H), 4.68 – 4.12 (m, 2H), 2.46 (d, J = 1.1 Hz, 3H), 1.79 (d, J = 0.7 Hz, 3H) ppm. ESI-MS m/z calc. 231.05746, found 232.0 (M+l) +; Retention time: 0.65 minutes.
At the same time, in my other blogs, there are other synthetic methods of this type of compound,105806-13-1, 4,6-Dichloro-5-fluoro-2-methylpyrimidine, and friends who are interested can also refer to it.
Reference:
Patent; VERTEX PHARMACEUTICALS INCORPORATED; COLLIER, Philip, N.; DAVIES, Robert, J.; DENINNO, Michael, Paul; DOYLE, Elisabeth; FRANTZ, James, Daniel; GOLDMAN, Brian, Anthony; GRILLOT, Anne-Laure; KOLPAK, Adrienne, Lynne; KRAUSS, Raul, Eduardo; LEDFORD, Brian; LIAO, Yusheng; MAGAVI, Sanjay, Shivayogi; MALTAIS, Francois; PEROLA, Emanuele; RYU, Elizabeth, Jin-Sun; SYKEN, Joshua; TANG, Qing; WANG, Tiansheng; (221 pag.)WO2018/106643; (2018); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia