反应详情

A mixture of 1.29 g of methyl 2-(5-bromopentanoylamino)-6-chloro-benzoate as synthesized in above Step 7-18-B, 800 mg of 2-piperazin-1-ylquinoline as synthesized in Step 7-1-A, 400 mg of triethylamine and 20 ml of toluene was heated under reflux for 3 hours. After cooling, the solution was washed with water, dried over anhydrous magnesium sulfate and the solvent was distilled off under reduced pressure. The residue was purified on silica gel column chromatography (ethyl acetate:methanol=15:1) to provide 1.13 g (64%) of methyl 2-chloro-6-[5-(4-quinolin-2-ylpiperazin-1-yl)pentanoylamino]benzoate.

1. temperaturewas heated
2. temperatureunder reflux for 3 hours
3. temperatureAfter cooling
4. washthe solution was washed with water
5. dry with materialdried over anhydrous magnesium sulfate
6. distillationthe solvent was distilled off under reduced pressure
7. customThe residue was purified on silica gel column chromatography (ethyl acetate:methanol=15:1)