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.641569-94-0, name is 4-Methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)benzoic acid, molecular formula is C17H14N4O2, molecular weight is 306.32, as common compound, the synthetic route is as follows.Safety of 4-Methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)benzoic acid
[00203] To a 1 liter reactor was fed 40 g of 4-methyl-3-(4-(pyridine-3-yl)pyrimidin- 2-ylamino)benzoic acid (0.13 mol), 200 ml of N-methyl pyrrolidone (NMP) (5V) and 13 ml of thionyl chloride (0.18 mol). The reactor was heated to 60C and maintained at 60C for 1.5 hr. After 1.5 hr of heating, 31.5 g of 3-(trifluoromethyl)-5-(4-methyl-lH-imidazol- 1 -yl)benzenamine (0.13 mol) was fed into the reactor. The reactor was then heated to 90C, and maintained for 30 minutes at this temperature. Then 200 ml (5 V) of water was added. The resulting mixture was maintained for 2 hours at 90C. Then, an additional 240 ml (6V) of N-methyl pyrrolidone was added, followed by 26.5 ml of sodium hydroxide (47% aqueous) to raise the pH to 6.5-7. The reactor was then cooled to 40C and maintained for 3 hours. The mixture was then filtered and the filter cake was washed with ethanol and water. The washed material was then dried in a vacuum tray oven overnight to provide dry Nilotinib base (62.1 g, Yield 90%)
At the same time, in my other blogs, there are other synthetic methods of this type of compound,641569-94-0, 4-Methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)benzoic acid, and friends who are interested can also refer to it.
Reference:
Patent; TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.; PIRAN, Maytal; RENDELL, Jacob; WO2011/163222; (2011); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem