反应详情

To a solution of 100 mg (0.225 mmol) of the oxadiazole from Example 23A in 1.5 ml of ethanol were added 383 mg (4.50 mmol) of 1-methylcyclobutanamine, and then the reaction mixture was stirred in the microwave at 80 for 2 h and then at 90° C. for 2 h. Another 383 mg (4.50 mmol) of 1-methylcyclobutanamine were added and the mixture was stirred in the microwave at 90° C. for a further 6 h and then at 100° C. for 6 h. Subsequently, another 383 mg (4.50 mmol) of 1-methylcyclobutanamine were added and the mixture was stirred in the microwave at 100 for a further 20 h. The solvent was removed under reduced pressure and the crude product was purified by means of preparative HPLC. Yield: 27.2 mg (24% of theory)

1. waitat 90° C. for 2 h
2. stirringthe mixture was stirred in the microwave at 90° C. for a further 6 h
3. waitat 100° C. for 6 h
4. stirringthe mixture was stirred in the microwave at 100 for a further 20 h
5. customThe solvent was removed under reduced pressure
6. customthe crude product was purified by means of preparative HPLC