反应详情

The above described pyridine derivative was converted into invention compound of Formula I by the addition of one equivalent of fumaric acid to a methanol (15 mL) solution of the free amine at 25° C. After 30 minutes the solvent was removed in vacuo and the residue pumped under high vacuum. Trituration with diethyl ether resulted in the formation of 5-(4-fluorophenyl)-3-(2-piperidinyl)pyridine fumarate (70%) as a colorless solid. M.p. 209°-210° C. (decomp., Et2O); 1H NMR (DMSO-d6, 300 MHz): δ8.86 (s, 1H), 8.63 (s, 1H), 8.32 (s, 1H), 7.81 (dd, J=8, 5 Hz, 2H), 7.32 (app. t, J=8 Hz, 2H), 6.49 (s, 2H), 4.24 (dd, J=10, 4 Hz, 1H), 3.37 (d, J=12 Hz, 1H), 2.97 (m, 1H), 1.5-2.1 (m, 6H).

1. customAfter 30 minutes the solvent was removed in vacuo