反应详情

The compound (140 mg, 0.41 mmol) prepared in Example 42 was dissolved in N,N-dimethylformamide (5 ml). 1,1′-Dicarbonyldiimidazole (73 mg, 0.45 mmol) was added thereto, and the mixture was stirred for 30 min at room temperature. N-hydroxy-cyclopentanecarboxamidine (260 mg, 2.03 mmol) was added thereto, and the mixture was stirred for 5 h at 80° C. After completion of the reaction, water was added. The mixture was extracted with ethyl acetate, dried over anhydrous magnesium sulfate, and filtered. The filtrate was distilled under reduced pressure, and purified by column chromatography to give the title compound (100 mg, Yield 56%).

1. stirringthe mixture was stirred for 5 h at 80° C
2. additionwas added
3. extractionThe mixture was extracted with ethyl acetate
4. dry with materialdried over anhydrous magnesium sulfate
5. filtrationfiltered
6. distillationThe filtrate was distilled under reduced pressure
7. custompurified by column chromatography