反应详情

温度

50 °C

A 3N aqueous solution of sodium hydroxide (0.694 ml) was added to methyl 2-[2-amino-5-[1-(1-tert-butoxycarbonyl-4-piperidyl)pyrazol-4-yl]-3-pyridyl]-1,3-benzoxazole-7-carboxylate (360 mg) dissolved in methanol (5 ml). The resulting solution was heated at 50° C. for 2 hours. The mixture was evaporated to dryness. Water (30 ml) was added and the pH was adjusted to 5 with dilute hydrochloric acid. The resultant solid was filtered, washed with water and dried under reduced pressure to afford 2-[2-amino-5-[1-(1-tert-butoxycarbonyl-4-piperidyl)pyrazol-4-yl]-3-pyridyl]-1,3-benzoxazole-7-carboxylic acid (320 mg) as yellow solid. NMR Spectrum: (DMSOd6) 1.46 (s, 9H), 1.80 (dd, 1H), 1.85 (dd, 1H), 2.00-2.09 (m, 2H), 2.93 (bs, 2H), 3.98-4.12 (m, 2H), 4.35-4.44 (m, 1H), 7.52 (dd, 1H), 7.63 (bs, 2H), 7.83 (s, 1H), 7.92 (d, 1H), 8.06 (d, 1H), 8.27 (s, 1H), 8.33 (d, 1H), 8.52 (d, 1H); Mass spectrum: M+H+ 505.

1. customThe mixture was evaporated to dryness
2. additionWater (30 ml) was added
3. filtrationThe resultant solid was filtered
4. washwashed with water
5. customdried under reduced pressure