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.1042986-00-4, name is 2-Fluoro-5-methylnicotinic acid, molecular formula is C7H6FNO2, molecular weight is 155.13, as common compound, the synthetic route is as follows.Recommanded Product: 2-Fluoro-5-methylnicotinic acid
Intermediate 9:2-fluoro-N-methoxy-N,5-dimethylnicotinamide[00366] To a solution of 2-fluoro-5-methylnicotinic acid (4.9 g, 31.6 mmol), N,O- dimethylhydroxylamine hydrochloride (4.01 g, 41.08 mmol), diisopropylethylamine (12.6 ml, 72.68 mmol) in dichloromethane (150 ml) at 0C was added TBTU (11.16 g, 34.76 mmol) portionwise over 30 minutes. The solution was stirred at 0C for a further 10 minutes then, at room temperature for 18 hours. The reaction mixture was washed with a 10wt% solution of citric acid and brine. The organic layer was dried over magnesium sulfate, filtered and concentrated in vacuo. The residue was purified on silica gel by flash column chromatography (ISCO Companion D, 8Og column, 0-20% EtOAc/Petrol) to afford the title compound as a colourless solid (5.44 g, 87% yield).[00367 ] 1H NMR (DMSO-d6, 400 MHz) delta 2.32 (3H, s), 2.69 (3H, s), 3.28 (3H, s), 7.92 (IH, dd), 8.15 (IH, s); MS (ES+) 199.
At the same time, in my other blogs, there are other synthetic methods of this type of compound,1042986-00-4, 2-Fluoro-5-methylnicotinic acid, and friends who are interested can also refer to it.
Reference:
Patent; VERTEX PHARMACEUTICALS INCORPORATED; WO2008/94992; (2008); A2;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem