With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.138498-97-2,2-(Tetrahydrofuran-3-yl)acetic acid,as a common compound, the synthetic route is as follows.
To a stirred solution of ethyl 1 -(6-(3, 5-difluoro-2-((2-methyl-4-(piperidin-4- yl)benzyl)oxy)phenyl)pyridin-2-yl)piperidine-4-carboxylate (500 mg, 0.910 mmol) in DMF (7 mL) stirred at 0C, were added 2-(tetrahydrofuran-3-yl)acetic acid (142 mg, 1.092 mmol) and BOP-CI (347 mg, 1.365 mmol). The reaction mixture was stirred at 0C for 30 minutes and then DIPEA (0.477 mL, 2.73 mmol) was added dropwise. The reaction mixture was stirred at 25 C for 12 hours and then was partitioned between water (10 ml) and EtOAc (20 ml). The organic phase was separated and the aqueous phase was further extracted with EtOAc (2×30 ml). The combined organic phase was washed with water (2×20 ml), dried over anhydrous Na2SO4 and then concentrated under reduced pressure. The crude product was purified by column chromatography (using 100-200 mesh silica gel, initially eluted with EtOAc/Hexane 10/90 to 20/80 to removed non-polar impurities, then with EtOAc/Hexane 8/2). The pure fractions were collected and concentrated under reduced pressure to afford the title compound (400 mg, 49.8 % yield) as a gummy solid.LCMS (a): Rt = 3.01 mi M/z = 662.34 (M+H)
138498-97-2, The synthetic route of 138498-97-2 has been constantly updated, and we look forward to future research findings.
Reference£º
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; BOUILLOT, Anne Marie Jeanne; DODIC, Nerina; (120 pag.)WO2016/42536; (2016); A1;,
Tetrahydrofuran – Wikipedia
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