反应详情

[(7-Cyclopentylamino-1H-indol-2-yl)-4,5-dihydro-thiazol-4-yl]acetic acid (140 mg, 0.41 mmol) prepared in Example 75 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°. After completion of the reaction, water was added. The reaction mixture was extracted with ethyl acetate, dried over anhydrous magnesium sulfate, and filtered. The filtrate was distilled under reduced pressure, and the residue was purified by column chromatography to give the title compound (100 mg, Yield 56%).

1. stirringthe mixture was stirred for 5 h at 80°
2. additionwas added
3. extractionThe reaction 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. customthe residue was purified by column chromatography