反应详情

温度

100 °C

A mixture of 210 mg of 1-cyclopropyl-7-(3-cyclopropyl-1-piperazinyl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid, 0.24 ml of 37% formaldehyde and 0.30 ml of 90% formic acid was heated at 100° C. for 4 hours, then allowed to cool and the excess reagents removed under reduced pressure. Water was added and the pH adjusted to 7 with 1N sodium hydroxide. The mixture was then extracted several times with chloroform:methanol (95:5), the extracts combined, dried, filtered and evaporated. The resulting oil was triturated with ether, giving 170 mg of the desired product.

1. temperatureto cool
2. customthe excess reagents removed under reduced pressure
3. additionWater was added
4. extractionThe mixture was then extracted several times with chloroform:methanol (95:5)
5. customdried
6. filtrationfiltered
7. customevaporated
8. customThe resulting oil was triturated with ether