Methanol → 1-(Pyridin-2-yl)piperidin-4-ol

Participants

Reaction Steps

1-(pyridin-2-yl)piperidin-4-ol (64.7% yield), 2-fluoropyridine (29.7 mmol, 2.88 g) and triethylamine (49.4 mmol, 6.89 ml, 5.00 g) were dissolved in MeOH (2.5 ml) and heated to 150° C. for 1 hour in the microwave. The solvent was removed at reduced pressure. The resulting residue was purified by column chromatography, eluting with DCM—3% MeOH/DCM to afford 1-(pyridin-2-yl)piperidin-4-ol. (1.14 g) 1H NMR (CDCl3) δ: 8.18 (d, 1H), 7.45 (m, 1H), 6.67 (d, 1H), 6.58 (m, 1H), 4.06 (m, 2H), 3.92 (br, 1H), 3.15 (m, 2H), 1.98 (m, 2H), 1.59 (m, 2H).

Provenance & Evidence