反应详情

Triethylamine (18 ml) was added to a suspension composed of 7-chloro-1,4-dihydro-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid ethyl ester (7.1 g) obtained in Example A-1 (4), trans-3-methoxy-4-methylaminopyrrolidine dihydrochloride (6.0 g) and acetonitrile (150 ml). The resulting reaction mixture was stirred at room temperature for 5 hours, and was then concentrated under reduced pressure. Then, an aqueous solution of sodium hydrogencarbonate was added, and the resultant mixture was extracted with chloroform. After the obtained extract was dried over anhydrous sodium sulfate, solvent was distilled off under reduced pressure, and the resultant residue was purified by silica gel column chromatography (eluent chloroform:methanol=6:1), and thus, there was obtained 1,4-dihydro-7-(trans-3-methoxy-4-methylamino-1-pyrrolidinyl)-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid ethyl ester (6.1 g).

1. customThe resulting reaction mixture
2. concentrationwas then concentrated under reduced pressure
3. additionThen, an aqueous solution of sodium hydrogencarbonate was added
4. extractionthe resultant mixture was extracted with chloroform
5. extractionAfter the obtained extract
6. dry with materialwas dried over anhydrous sodium sulfate, solvent
7. distillationwas distilled off under reduced pressure
8. customthe resultant residue was purified by silica gel column chromatography (eluent chloroform:methanol=6:1)