反应详情

A RBF was charged with (E)-ethyl 3-(5-(benzylthio)-2-((4-bromo-5-chloro-2-methoxyphenyl)amino)-4-fluorophenyl)acrylate (1.80 g, 3.27 mmol) and MeOH (16.3 ml) to give a yellow suspension. Sodium methoxide (25 wt % in MeOH) (0.291 ml, 1.307 mmol) was added. A reflux condenser was attached, and the flask was lowered into a 70° C. heating bath. After 16 h, the mixture was cooled and concentrated under vacuum. The residue was triturated with 2-PrOH and filtered to give 6-(benzylthio)-1-(4-bromo-5-chloro-2-methoxyphenyl)-7-fluoroquinolin-2(1H)-one (1.23 g, 2.44 mmol, 74.6% yield) as a tan solid. m/z (ESI) 504.0 (M+H)+.

1. customto give a yellow suspension
2. customA reflux condenser was attached
3. customwas lowered into a 70° C.
4. temperatureheating bath
5. temperaturethe mixture was cooled
6. concentrationconcentrated under vacuum
7. customThe residue was triturated with 2-PrOH
8. filtrationfiltered