反应详情

Add trifluoroacetic acid (1.5 mL) to a solution of tert-butyl 5-[5-[2-(indan-2-ylamino)-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-5-oxo-pentyl]imidazole-1-carboxylate (0.030 g; 0.058 mmoles) in dichloromethane (8 mL). Stir the reaction at room temperature for 2 hr. Concentrate the mixture and add saturated sodium bicarbonate (10 mL) and water (20 mL), then extract with dichloromethane (3×20 mL). Wash the combined organic extracts with brine, dry over sodium sulfate, filter, and concentrate. Purify the crude product by column chromatography (0 to 10% methanol in dichloromethane) to afford 1-[2-(2,3-dihydro-1H-inden-2-ylamino)-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl]-5-(1H-imidazol-4-yl)pentan-1-one (0.020 g; 83%) as a white solid: MS (m/z): 417 (M+1).

1. customthe reaction at room temperature for 2 hr
2. concentrationConcentrate the mixture
3. additionadd saturated sodium bicarbonate (10 mL) and water (20 mL)
4. extractionextract with dichloromethane (3×20 mL)
5. washWash the combined organic extracts with brine
6. dry with materialdry over sodium sulfate
7. filtrationfilter
8. concentrationconcentrate
9. customPurify the crude product by column chromatography (0 to 10% methanol in dichloromethane)