Synthesis
At room temperature, 2-(4,4-difluoropiperidin-1-yl)acetonitrile (480 mg, 3.0 mmol) was dissolved in tetrahydrofuran (THF, 10 mL), followed by addition of lithium aluminum hydride (LAH, 228 mg, 6.0 mmol). The reaction mixture was stirred overnight at room temperature and then quenched by slow addition of water (10 mL) and 15% aqueous sodium hydroxide (10 mL). The resulting mixture was filtered and the filtrate was concentrated under reduced pressure to give the crude product. The crude product was purified by column chromatography (dichloromethane: methanol = 10:1) to afford 2-(4,4-difluoropiperidin-1-yl)ethylamine (400 mg, 80% yield) as a yellow oil.
References
[1] Patent: WO2014/182829, 2014, A1. Location in patent: Page/Page column 131
[2] Patent: WO2015/131080, 2015, A1. Location in patent: Paragraph 00534; 00536
[3] Patent: US2006/58308, 2006, A1. Location in patent: Page/Page column 46
[4] Bioorganic and Medicinal Chemistry Letters, 2011, vol. 21, # 1, p. 497 - 501
[5] Patent: WO2015/150449, 2015, A2. Location in patent: Page/Page column 204
