Electric Literature of 403-45-2 ,Some common heterocyclic compound, 403-45-2, molecular formula is C6H4FNO2, 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.
Methyl 6-fluoronicotinate. To a solution of 6-fluoronicotinic acid (255 mg, 1.32 mmol) in methanol (5 mL) at room temperature was added (trimethylsilyl)diazomethane (4.0 mL, 2 M in diethyl ether, 8.0 mmol). The reaction mixture was stirred at room temperature for 30 min and concentrated. Methyl 6- fluoronicotinate (129 mg, 47%) was used without further purification: 1H NMR (600 MHz, DMSOd6) delta 8.79 (d, J = 2.6 Hz, IH), 8.47 (td, J = 7.9, 2.6 Hz, IH), 7.35 (ddd, J = 8.5, 2.6, 0.6 Hz, IH), 3.88 (s, 3H); ESIMS calcd 156.0 (M+ + H), found 156.1 (M+ + H).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,403-45-2, its application will become more common.
Reference:
Patent; MERCK & CO., INC.; ATON PHARMA, INC.; WO2007/2248; (2007); A2;,
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