Ethanol → Ethyl 5-aminopyridine-2-carboxylate

関与物質

反応手順

To a solution of 5-aminopicolinic acid (13.5 g, 97.7 mmol) in anhydrous ethanol (200 mL) was added SOCl2 (60.0 mL, 504 mmol) dropwise at 0° C. under N2 atmosphere. The resulting mixture was heated at reflux and stirred overnight. The reaction mixture was concentrated in vacuo. The residue was dissolved in a saturated aqueous NaHCO3 solution so that that pH of the solution was approximately pH 9-10. The reaction mixture was extracted with EtOAc (8×250 mL). The combined organic phases were dried over Na2SO4, filtered, and the filtrate was concentrated in vacuo to afford the title compound as a brown solid (14.3 g, 88%)

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