Analyzing the synthesis route of Methyl 5-(trifluoromethyl)picolinate

At the same time, in my other blogs, there are other synthetic methods of this type of compound,124236-37-9, Methyl 5-(trifluoromethyl)picolinate, and friends who are interested can also refer to it.

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.124236-37-9, name is Methyl 5-(trifluoromethyl)picolinate, molecular formula is C8H6F3NO2, molecular weight is 205.134, as common compound, the synthetic route is as follows.COA of Formula: C8H6F3NO2

IV. (5-trifluoromethyl-2-pyridinyl)methanol To a solution of methyl 5-trifluoromethyl-pyridine-2-carboxylate (2 g, 9.75 mmol) in MeOH (30 mL) at 0C was added NaB (738 mg, 19.5 mmol) portionwise. The mixture was stirred at room temperature for 2 h and concentrated. The residue was diluted with water (30 mL), acidified to pH~5 (IN HC1), extracted with EA (3 X 50 mL), dried, concentrated and purified by column chromatography on silica gel to give the title compound as a colorless oil (1.6 g, 93% yield): 1H NMR (400 MHz, CDC13) delta ppm 8.82 (s, 1H), 7.90-7.92 (m, 1H), 7.40-7.42 (m, 1H), 4.82-4.83 (m, 2H), 3.44-3.46 (m, 1H); ES-LCMS m/z 178 ( +H)+.

At the same time, in my other blogs, there are other synthetic methods of this type of compound,124236-37-9, Methyl 5-(trifluoromethyl)picolinate, and friends who are interested can also refer to it.

Reference:
Patent; GLAXOSMITHKLINE LLC; QIN, Donghui; CHRISTENSEN, IV, Siegfried Benjamin; WU, Chengde; ZHANG, Zhiliu; YU, Haiyu; YUAN, Jiangxing; LIN, Xiaojuan; XU, Shanli; LV, Maoyun; YAO, Chen; LI, Lei; HUANG, Xing; GAO, Min; WO2013/166621; (2013); A1;,
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