Synthesis
General procedure for the synthesis of 2-fluoro-5-aminopyridine from 2-fluoro-5-nitropyridine: 50 mL of toluene and 50 mmol of 2-fluoro-5-nitropyridine were added to a 100 mL round-bottomed flask, followed by 0.282 g of 5% Pd/C catalyst and 10 mmol of anhydrous sodium sulfate. The reaction system was placed under hydrogen atmosphere, heated and stirred for 15 hours. Upon completion of the reaction, the mixture was cooled to room temperature, the catalyst was removed by filtration and the filtrate was concentrated by rotary evaporation. The resulting crude product was purified by recrystallization and finally dried under vacuum to give 1.6806 g of 2-fluoro-5-aminopyridine solid in 75% yield.
References
[1] Journal of the Chemical Society - Perkin Transactions 1, 1996, # 18, p. 2221 - 2226
[2] Patent: CN103755744, 2016, B. Location in patent: Paragraph 0065; 0066
[3] Bioorganic and Medicinal Chemistry Letters, 2004, vol. 14, # 6, p. 1411 - 1416
[4] Patent: US6355636, 2002, B1. Location in patent: Page column 64
[5] Patent: EP1171440, 2004, B1. Location in patent: Page 53
