Extracurricular laboratory: Synthetic route of 5-Bromo-2-fluoropyrimidine

The chemical industry reduces the impact on the environment during synthesis 62802-38-4, I believe this compound will play a more active role in future production and life.

Electric Literature of 62802-38-4, 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.62802-38-4, name is 5-Bromo-2-fluoropyrimidine, molecular formula is C4H2BrFN2, molecular weight is 176.9745, as common compound, the synthetic route is as follows.

[00378] 65A: 2-fluoro-5-(2-fluoro-5-methoxyphenyl)pyrimidine. To a stirred solution of 5-bromo-2-fluoropyrimidine (707 mg, 3.99 mmol) in Toluene (5.0 mL) was added (2- fluoro-5-methoxyphenyl)boronic acid (815 mg, 4.79 mmol), tetrakis(triphenylphosphine) palladium(O) (231 mg, 0.200 mmol) and potassium carbonate (1656 mg, 1 1.98 mmol). The resulting mixture was purged with argon and stirred at 1 10 C for 16h. After cooled to room temperature, the reaction mixture was diluted with water and extracted with DCM. The combined organic extracts were dried over sodium sulfate, filtered and concentrated to give a solid which was purified by chromatography to afford 2-fluoro-5- (2-fluoro-5-methoxyphenyl)pyrimidine (265 mg, 1.169 mmol, 29.3 % yield) as a white solid. LC-MS Anal.Calc’d for CuH8F2N20 222.06, found [M+H] 223.0.

The chemical industry reduces the impact on the environment during synthesis 62802-38-4, I believe this compound will play a more active role in future production and life.

Reference:
Patent; BRISTOL-MYERS SQUIBB COMPANY; HERNANDEZ, Andres S.; ELLSWORTH, Bruce A.; EWING, William R.; CHEN, Bin; WO2014/78608; (2014); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia