反应详情

To a suspension of NaH in DMF with ice bath cooling is added di-t-butyl malonate. After the addition, 8-chloro-1-cyclopropyl-7-fluoro-9-methyl-4-oxo-4H-quinolizine-3-carboxylic acid ethyl ester from Example 253i above is added. The reaction is then heated to 50° to 60° C., and the mixture is poured into water and acidified. The product is extracted into methylene chloride and dried over MgSO4. The residue, after removal of the solvent, is dissolved in methylene chloride and trifluoroacetic acid at room temperature. The solvent is removed under vacuum, and the product is treated with diphenyldiazomethane in methylene chloride and methanol. When the reaction is finished, the solvents are removed under vacuum, and the product is purified by column chromatography to give the title compound.

1. temperaturecooling
2. additionabove is added
3. temperatureThe reaction is then heated to 50° to 60° C.
4. extractionThe product is extracted into methylene chloride
5. dry with materialdried over MgSO4
6. customThe residue, after removal of the solvent
7. dissolutionis dissolved in methylene chloride
8. customat room temperature
9. customThe solvent is removed under vacuum
10. additionthe product is treated with diphenyldiazomethane in methylene chloride and methanol
11. customthe solvents are removed under vacuum
12. customthe product is purified by column chromatography