反应详情

300 mg of 1cyclopropyl-6,7-difluoro-8-chloro-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid, 530 mg of t-butyl 8-(methoxyimino)-2,6-diazaspiro[3,4]octane-2-carboxylate and 2 g of Amberlite® IRA-420 were added to 10 ml of acetonitrile and thereto 1 ml of triethylamine was added by dropping. The resulting mixture was refluxed for 72 hours and then the resulting solid was filtered off. The filtrate was concentrated under the reduced pressure and thereto 10 ml of ethylacetate was added and the resulting solution was stirred for 4 hours. The precipitated solid was filtered and dried to give 169 mg of the titled compound(yield: 31.4%).

1. temperatureThe resulting mixture was refluxed for 72 hours
2. filtrationthe resulting solid was filtered off
3. concentrationThe filtrate was concentrated under the reduced pressure
4. addition10 ml of ethylacetate was added
5. filtrationThe precipitated solid was filtered
6. customdried