反应详情

5-[2-fluoro-4-(1H-tetrazol-1-yl)phenyl]-2-(piperidin-4-yl)benzo[d]oxazole 2,2,2-trifluoroacetate (50 mg) was dissolved in DCM (15 ml) and added TEA (0.3 ml). This mixture stirred for 3 h at rt. Work up (DCM/H2O) followed by purification of the crude by preparative TLC using MeOH and DCM (1:5) as eluent afforded the titled compound (15 mg) as an off-white solid. M.P.: 148-151° C. 1H-NMR (δ ppm, DMSO-d6, 400 MHz): 10.17 (s, 1H), 8.03 (d, J 9.6, 1H), 7.95-7.79 (m, 4H), 7.58 (d, J 8.5, 1H), 3.22-3.13 (m, 1H), 3.07 (d, J 12.4, 2H), 2.70 (t, J 11.2, 2H), 2.06 (d, J 11.1, 2H), 1.82-1.70 (m, 2H).

1. customfollowed by purification of the crude by preparative TLC