反应详情

To a solution consisting of lithium hydroxide monohydrate (0.13 g, 3.0 mmol) dissolved in ethanol (10 mL)/water (5 mL) was added ethyl 5-(2-phenoxypyrimidin-5-yl)-1H-pyrazole-3-carboxylate (Example 54, 90 mg, 0.29 mmol) and the mixture was stirred at room temperature for 18 hours. Ethanol was removed under reduced pressure and the solution diluted with water and subsequently was acidified with acetic acid to precipitate product. The solid precipitate was filtered, washed with water, and dried under high vacuum to afford the title compound as a white solid (64 mg, 79% yield); Rf 0.15 with 2% methanol in dichloromethane; 1H-NMR (300 MHz; DMSO-d6) δ 9.12 (s, 2H), 7.49 (dd, 2H), 7.25-7.43 (m, 4H); MS (ESI−) m/z 281 (M−1); H-PGDS FPBA IC50: 5 μM.

1. customEthanol was removed under reduced pressure
2. additionthe solution diluted with water
3. customto precipitate product
4. filtrationThe solid precipitate was filtered
5. washwashed with water
6. customdried under high vacuum