反应详情

温度

120 °C

To the suspension of 4-methoxy-6-[4-oxo-2-((1R,2S)-2-phenyl-cyclopropylamino)-4H-thiazol-(5Z)-ylidenemethyl]-quinoline-3-carboxylic acid methyl ester (example 1) (50 mg, 0.11 mmol) in chloroform (5 mL) was added dimethylethylenediamine (0.048 mL, 0.44 mmol). The mixture was stirring at 120° C. for 3 h. After cooling, the solid was collected by filtration and washed with methylenechloride. The solid was dissolved in acetonitrile and 1N hydrochloride acid (0.22 mL, 0.22 mmol) was added. The resulting solution was lyophilized to give 4-methoxy-6-[4-oxo-2-((1R,2S)-2-phenyl-cyclopropylamino)-4H-thiazol-(5Z)-ylidenemethyl]-quinoline-3-carboxylic acid (2-dimethylamino-ethyl)-amide; hydrochloride. LC-MS m/e 516 (MH+).

1. temperatureAfter cooling
2. filtrationthe solid was collected by filtration
3. washwashed with methylenechloride
4. dissolutionThe solid was dissolved in acetonitrile