反应详情

To a solution of ethyl 1-[(4-{5-[4-phenyl-5-(trifluoromethyl)-2-thienyl]-1,2,4-oxadiazol-3-yl}-2-thienyl)methyl]azetidine-3-carboxylate (70 mg, 0.13 mmol) that was obtained in Example 3 (3d) in dioxane (2 ml) was added a 1N aqueous solution of sodium hydroxide (0.39 ml, 0.39 mmol) with stirring, and the resulting mixture was stirred at room temperature for 2 hours. After stirring, acetic acid (22 μl, 0.39 mmol) was added to the reaction mixture to quench the reaction, and the resulting mixture was evaporated in vacuo. To the residue thus obtained were added successively methanol (1 ml) and water (1 ml) with stirring, and the white solid precipitated was collected by filtration using a Kiriyama funnel, washed with a mixed solvent of water and methanol (3:7) and dried in vacuo to afford the title compound (34 mg) in a yield of 53% as a crystalline white solid.

1. stirringthe resulting mixture was stirred at room temperature for 2 hours
2. stirringAfter stirring
3. customto quench
4. customthe reaction
5. customthe resulting mixture was evaporated in vacuo
6. customTo the residue thus obtained
7. stirringwith stirring
8. customthe white solid precipitated
9. filtrationwas collected by filtration
10. washwashed with a mixed solvent of water and methanol (3:7)
11. customdried in vacuo