Synthetic Route of 884495-03-8 ,Some common heterocyclic compound, 884495-03-8, molecular formula is C5H4BrFN2, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route.
Step 1: 3-Amino-5-fluoro-pyridine-2-carboxyilic acid methyl ester: [00308] A solution of 3-amino-2-bromo-5-fluoropyridine (CAS: 884495-03-8, 955 mg, 5 mmol) and Pd(dppf)Cl2?CH2Cl2 (204 mg, 25 mmol) in dry MeOH (15 mL) and DIEA (1.74 mL, 10 mmol) was flushed with N2 after which a pressure of 8 atm CO was applied. The reaction was heated at 70 C. After completion, the mixture was diluted with water and extracted with EtOAc. The combined organic fractions were washed with NH4Cl solution, dried over Na2SO4, filtered and concentrated. The obtained residue was purified by column chromatography eluted using a mixture of EtOAc and petroleum ether (25:75). The obtained titled compound was used as such.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,884495-03-8, its application will become more common.
Reference:
Patent; ABBVIE S.A.R.L.; GALAPAGOS NV; ALTENBACH, Robert, J.; COWART, Marlon, D.; DE MUNCK, Tom, Roger Lisette; DROPSIT MONTOVERT, Sebastien Jean, Jacques Cedric; GFESSER, Gregory, A.; KELGTERMANS, Hans; MARTINA, Sebastien, Laurent Xavier; VAN DER PLAS, Steven, Emiel; WANG, Xueqing; (300 pag.)WO2016/193812; (2016); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem