(6-Piperdin-1-ylpyridin-3-yl)Methyl aMine synthesis

Yield:914637-06-2 111 mg

Reaction Conditions:

with lithium aluminium tetrahydride in diethyl ether at 20; for 2.5 h;Cooling with ice;Inert atmosphere;

Steps:

85 Reference Example 85

To a solution of 6-(piperidin-1-yl)nicotinonitrile (108 mg) in diethyl ether (15 mL), lithium aluminum hydride (66 mg) was added under ice cooling, and the mixture was stirred at room temperature for 2 hours and 30 minutes in a nitrogen atmosphere. To the reaction mixture, ethyl acetate and water were added under ice cooling, followed by separation of an organic layer. An aqueous layer was extracted twice with ethyl acetate, combined with the organic layer, washed with a saturated aqueous solution of sodium chloride and then dried over sodium sulfate, and the solvent was distilled off under reduced pressure to obtain a white solid of 1-(6-(piperidin-1-yl)pyridin-3-yl)methanamine (111 mg). ¹H-NMR (CDCl₃) δ value: 1.59-1.70 (m, 6H), 3.46-3.56 (m, 4H), 3.73 (s, 2H), 6.65 (d, J=8.8 Hz, 1H), 7.44 (dd, J=8.6, 2.3 Hz, 1H), 8.09 (d, J=2.2 Hz, 1H).

References:

EP2810944,2014,A1 Location in patent:Paragraph 0432-0433