Synthetic Route of 884495-03-8, 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.884495-03-8, name is 3-Amino-2-bromo-5-fluoropyridine, molecular formula is C5H4BrFN2, molecular weight is 191.0011, as common compound, the synthetic route is as follows.
3-amino-2-bromo-5-fluoropyridine 84A (25 g, 131 mmol, Astatech Chemical, Inc) was treated with ZnCN2 (16.9 g, 1.1 equiv., 144 mmol), Pd(Ph3)4(11.3 g, 0.075 equiv., 9.8 mmol) and DMF (200 mL) and then heated to 115 C. After 6 h, the reaction mixture was allowed to cool and then concentrated under reduced pressure to a solid. The solid was washed with EtOAc (2¡Á100 mL). The organic layers were combined and washed with water (3¡Á100 mL), saturated NH4Cl solution (100 mL), dried over MgSO4, filtered and concentrated under reduced pressure to provide 84B that was used without further purification. LCMS (m/z): 138.87 [M+H]+; tR=0.59 min. on LC/MS Method A.
The chemical industry reduces the impact on the environment during synthesis 884495-03-8, I believe this compound will play a more active role in future production and life.
Reference:
Patent; Gilead Sciences, Inc.; Aktoudianakis, Evangelos; Chin, Gregory; Mackman, Richard L.; Metobo, Samuel E.; Mish, Michael R.; Pyun, Hyung-jung; Zablocki, Jeff; (175 pag.)US2016/289229; (2016); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem