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.1052714-46-1, name is 6-Bromo-5-fluoropicolinic acid, molecular formula is C6H3BrFNO2, molecular weight is 219.9959, as common compound, the synthetic route is as follows.Recommanded Product: 1052714-46-1
[0273] 6-Bromo-5-fluoro-pyridine-2-carboxylic acid (24.0 g, 109 mmol) was dissolved in a mixture of EtOH (400mL) and cone. H2SO4 (17.5 mL, 328 mmol). The mixture was heated at 90 C for 2.5 h. After cooling to 0 C, a solution of 3.50 M NaOH (90.0 mL, 315 mmol) was slowly added with vigorous stirring (pH adjusted to approx. 4), followed by a sat. solution of NaHC03 until pH was approx. 8. The slurry was filtered through a pad of Celite, and the filtrate was concentrated under reduced pressure. The residue was suspended in cold water (300 mL) and stirred at 0 C for 5 m. The mixture was filtered, washing with water, and the solid was dried under vacuum to provide the title compound as a solid (20.4 g, 75%). XH NMR (500 MHz, (0777) CDC13) delta 8.12 (dd, J = 8.3, 3.6 Hz, 1H), 7.53 (dd, J = 8.3, 7.0 Hz, 1H), 4.47 (q, J = 7.1 Hz, 2H), 1.43 (t, J = 7.1 Hz, 3H). LC-MS (Method C): m/z (ES+), [M+H]+ = 247.8. HPLC tR = 1.74 m.
At the same time, in my other blogs, there are other synthetic methods of this type of compound,1052714-46-1, 6-Bromo-5-fluoropicolinic acid, and friends who are interested can also refer to it.
Reference:
Patent; ASTRAZENECA AB; CUMMING, John, Graham; WU, Frank, Xinhe; EDMAN, Karl, Henrik; CHEN, Hongming; BROWN, Dean, Gordon; BURLI, Roland, Werner; JOHNSTONE, Shawn, Donald; BROWN, Giles, Albert; TEHAN, Benjamin, Gerald; TEOBALD, Barry, John; CONGREVE, Miles, Stuart; (187 pag.)WO2017/194716; (2017); A1;,
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