反应详情

温度

70 °C

To a vial containing 5-tert-butyl-2-aminothiophene-3-carboxylic acid (1 mmol) in THF (7 mL) was added 2,3-dichlorophenyl isocyanate (1 mmol). The vial was capped and the solution was stirred at 70° C. for 21 hours. The reaction was cooled down to room temperature and the solvent was removed under vacuum. The oil residue was treated with dichloromethane and the resulting mixture was left to stand at room temperature for 1 hour. The solids were filtered, washed with minimal amount of dichloromethane and dried under vacuum to yield the expected 5-tert-butyl-2-(3-(2,3-dichlorophenyl)ureido)thiophene-3-carboxylic acid (317.2 mg, 83%). Coupling with the appropriate amine was performed as described above for Example 1.

1. customThe vial was capped
2. temperatureThe reaction was cooled down to room temperature
3. customthe solvent was removed under vacuum
4. additionThe oil residue was treated with dichloromethane
5. waitthe resulting mixture was left
6. waitto stand at room temperature for 1 hour
7. filtrationThe solids were filtered
8. washwashed with minimal amount of dichloromethane
9. customdried under vacuum