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.7598-35-8, name is 2-Bromopyridin-4-amine, molecular formula is C5H5BrN2, molecular weight is 173.01, as common compound, the synthetic route is as follows.HPLC of Formula: C5H5BrN2
To a 3-necked round-bottom flask containing 2-bromopyridin-4-amine (100 g, 578 mmol), acetic acid (1 L) and sodium acetate (118 g, 1.44 mol) was added a solution of iodine monochloride (103 g, 635 mmol) in acetic acid (0.5 L) dropwise with stirring at 50 C. The resulting solution was stirred for 3 h at 75 C. The reaction mixture was cooled to room temperature and concentrated in vacuo. The resulting solution was diluted with brine (1 L) and extracted with EtOAc (3 x 1 L). The combined organic layers were washed with saturated aqueous sodium bicarbonate (2 x 0.5 L), saturated aqueous sodium sulfite (0.2 L), and brine (0.3 L), dried over anhydrous sodium sulfate and concentrated in vacuo. The crude product was purified via flash chromatography on silica gel (eluent: 5% EtOAc in dichloromethane) to afford 2-bromo-5-iodopyridin-4-amine (50 g, 29%) as a white solid. LCMS (ESI): RT (min) = 1.114, [M+H]+ = 299, method = L.
At the same time, in my other blogs, there are other synthetic methods of this type of compound,7598-35-8, 2-Bromopyridin-4-amine, and friends who are interested can also refer to it.
Reference:
Patent; GENENTECH, INC.; BRYAN, Marian C.; CHAN, Bryan; DIEDERICH, Francois; DOTSON, Jennafer; HANAN, Emily; HEFFRON, Timothy; LAINCHBURY, Michael; HEALD, Robert; SEWARD, Eileen M.; WO2014/210354; (2014); A1;,
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