反应详情

A solution of methyl 5-(3,3-difluoroazetidin-1-yl)-6-(2-fluoroethoxyl)pyridine-2-carboxylate (Example 147 b, 73 mg, 252 μmol) and lithium hydroxide hydrate (12.7 mg, 302 μmol) in tetrahydrofuran (500 μL) and water (50.0 μL) was stirred for 12 h at ambient temperature. The reaction mixture was poured onto ice/0.1 N HCl (25 mL) and extracted with EtOAc (2×25 mL). The combined extracts were washed with ice/brine (25 mL), dried over Na2SO4, filtered and evaporated to dryness to give the target compound (69 mg, quant.) as off-white solid, MS (ESI) m/e=277.1 [MH+].

1. additionThe reaction mixture was poured onto ice/0.1 N HCl (25 mL)
2. extractionextracted with EtOAc (2×25 mL)
3. washThe combined extracts were washed with ice/brine (25 mL)
4. dry with materialdried over Na2SO4
5. filtrationfiltered
6. customevaporated to dryness
7. customto give the target compound (69 mg, quant.) as off-white solid, MS (ESI) m/e=277.1 [MH+]