反应详情

温度

0 °C

[(R)-2-(5-chloro-7-cyclopentylamino-1H-indol-2-yl)-4,5-dihydro-thiazol-4-yl]-acetic acid (391 mg, 1 mmol) prepared in Example 4 was dissolved in DCM (10 mL). Triethylamine (280 ul, 2 mmol) and isobutyric acid chloride (106 mg, 1 mmol) were added thereto, and the mixture was stirred for 30 min at 0° C. After completion of the reaction, the solvent was removed under reduced pressure. The residue was diluted with THF. NaBH4 (74 mg, 2 mmol) was added thereto, and the mixture was stirred for 12 h. The reaction was quenched with a small amount of water. Again, excess water was added to the reaction mixture, which was then stirred for 30 min, extracted with EtOAc, dried over MgSO4, and filtered. The solvent was removed under reduced pressure, and the residue was purified by column chromatography to give the title compound (272 mg, Yield 72%).

1. customAfter completion of the reaction
2. customthe solvent was removed under reduced pressure
3. additionThe residue was diluted with THF
4. stirringthe mixture was stirred for 12 h
5. customThe reaction was quenched with a small amount of water
6. additionAgain, excess water was added to the reaction mixture, which
7. stirringwas then stirred for 30 min
8. extractionextracted with EtOAc
9. dry with materialdried over MgSO4
10. filtrationfiltered
11. customThe solvent was removed under reduced pressure
12. customthe residue was purified by column chromatography