Each compound has different characteristics, and only by selecting the characteristics of the compound suitable for a specific situation can the compound be applied on a large scale. 884495-30-1, name is 5-Fluoro-2-methoxyisonicotinic acid. This compound has unique chemical properties. The synthetic route is as follows. Application In Synthesis of 5-Fluoro-2-methoxyisonicotinic acid
(5-Fluoro-2-methoxy-pyridin-4-yl)methanol, used as starting material was prepared as follows:-Borane-tetrahydrofuran complex (1M solution in THF, 52.6 ml, 52.6 mmol) was added slowly to a solution of 5-fluoro-2-methoxy-pyridine-4-carboxylic acid (2 g, 11.7 mmol) in THF (100 ml) under nitrogen. The reaction mixture was stirred at room temperature for 2.5 h. The solvent was then evaporated and the residue was stirred in methanol (40 ml) for 16 h. The solvent was evaporated and the residue was purified on a silica isolute column, eluting with 0-1% MeOH in DCM to afford (5-fluoro-2-methoxy-pyridin-4-yl)methanol as a white solid (1.42 g, 77% yield).1H NMR (399.902 MHz, CDCl3) delta 3.90 (s, 3H), 4.76 (s, 2H), 6.84-6.87 (m, 1H), 7.92 (d, 1H). MS: m/z 158 (MH+); (5-Fluoro-2-methoxy-pyridin-4-yl)methanol, used as starting material, was prepared as follows:-Borane-tetrahydrofuran complex (IM solution in THF, 52.6 ml, 52.6 mmol) was added slowly to a solution of 5-fluoro-2-methoxy-pyridine-4-carboxylic acid (2 g, 11.7 mmol) in THF (100 ml) under nitrogen. The reaction mixture was stirred at room temperature for 2.5 h. The solvent was evaporated and the residue was stirred in methanol (40 ml) for 18 h. The solvent was evaporated and the crude product was purified by silica column chromatography, eluting with 0-1% MeOH in DCM. Pure product fractions were combined and evaporated to afford (5-fluoro-2-methoxypyridin-4-yl)methanol as a white solid (1.42 g, 77%).1H NMR (399.902 MHz, CDCl3) delta 3.90 (s, 3H), 4.76 (s, 2H), 6.84-6.87 (m, 1H), 7.92 (d, 1H); m/z (ES+) [M+H]+=158.
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Reference:
Patent; ASTRAZENECA AB; US2008/4302; (2008); A1;,
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