The origin of a common compound about 2,4,6-Trichloro-5-fluoropyrimidine

At the same time, in my other blogs, there are other synthetic methods of this type of compound,6693-08-9, 2,4,6-Trichloro-5-fluoropyrimidine, and friends who are interested can also refer to it.

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.6693-08-9, name is 2,4,6-Trichloro-5-fluoropyrimidine, molecular formula is C4Cl3FN2, molecular weight is 201.4136, as common compound, the synthetic route is as follows.Formula: C4Cl3FN2

2,6-Dichloro-5-fluoro-Lambda/-(l-methyl-lH-imidazol-4-yl)pyrimidin-4-amine l-Methyl-4-nitro-lH-imidazole (Intermediate 5, 500 mg, 3.93 mmol) was dissolved in ethanol (6.771 mL) and Pd/C (10 wt%, Degussa, 105 mg, 0.10 mmol) was added. The reaction was subjected to 1 atm of hydrogen for 3 hours. TLC indicated that the reaction was completed, and the reaction mixture was filtered through Celite. The filtrate was cooled to 00C and TEA (1.097 mL, 7.87 mmol) and 2,4,6-trichloro-5-fluoropyrimidine (obtained via the procedure described in PCT Pub. No. WO2008/132502, 792 mg, 3.93 mmol) were added. The reaction was allowed to warm to room temperature slowly overnight. The reaction mixture was filtered providing the title compound as a yellow solid (820 mg) with 95% purity. LCMS: 263 [M+Eta]+.

At the same time, in my other blogs, there are other synthetic methods of this type of compound,6693-08-9, 2,4,6-Trichloro-5-fluoropyrimidine, and friends who are interested can also refer to it.

Reference:
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; ALMEIDA, Lynsie; CHUAQUI, Claudio, Edmundo; GUAN, Amy; IOANNIDIS, Stephanos; LAMB, Michelle; PENG, Bo; SU, Qibin; WO2010/20810; (2010); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia