反应详情

温度

60 °C

tert-Butyl 2-oxo-8-(2-oxopyrrolidin-1-yl)-1-(thiophen-3-ylmethyl)-1,2,3,4-tetrahydroquinolin-3-ylcarbamate (399 g) was suspended in ethanol (2 L), and concentrated hydrochloric acid (555 mL) was added to the suspension, followed by stirring at 60° C. for 30 minutes. The reaction mixture was neutralized with 25% aqueous sodium hydroxide solution under cooling on ice. The resultant mixture was partitioned between chloroform and water, and the aqueous layer was extracted with chloroform. The organic layers were combined, and the combined organic layer was dried over sodium sulfate. The solvent was evaporated under reduced pressure, whereby the title compound (418 g) in a crude form was yielded, which was employed in the subsequent reaction step without performing further purification.

1. temperatureunder cooling on ice
2. customThe resultant mixture was partitioned between chloroform and water
3. extractionthe aqueous layer was extracted with chloroform
4. dry with materialthe combined organic layer was dried over sodium sulfate
5. customThe solvent was evaporated under reduced pressure, whereby the title compound (418 g) in a crude form
6. customwas yielded
7. customwhich was employed in the subsequent reaction step
8. custompurification