反应详情

温度

100 °C

To 1.57 g (5 mmol) of 5-amino-8-chloro-1-cyclo- propyl-6,7-difluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acid in 20 ml of acetonitrile was added 0.93 g (5 mmol) of 3-[(t-butoxycarbonyl)amino]pyrrolidine and 1.0 g (10 mmol) of triethylamine. The mixture was refluxed for three hours, cooled, and filtered. The solids were washed with acetonitrile and ether, then dissolved in 10 ml of acetic acid and 2 ml of 3 N hydrochloric acid. The mixture was heated at 100° C. for four hours, concentrated, and triturated with 2-propanol. The solid that formed was filtered and washed with ether to give 1.2 g of the title compound.

1. temperatureThe mixture was refluxed for three hours
2. temperaturecooled
3. filtrationfiltered
4. washThe solids were washed with acetonitrile and ether
5. dissolutiondissolved in 10 ml of acetic acid
6. concentrationconcentrated
7. customtriturated with 2-propanol
8. customThe solid that formed
9. filtrationwas filtered
10. washwashed with ether