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HRID 25175作成日:2026年10月26日

Diisopropyl Ether → 1-(6-Amino-3,5-difluoropyridin-2-yl)-8-bromo-7-(3-ethylaminoazetidin-1-yl)-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid

https://huagongshe.com/reaction/25175

反応式

関与物質

役割名称HCID仕込み量
反応物Diisopropyl EtherHCID 7914—
反応物1-MethylpyrrolidineHCID 8454—
反応物N-ethylazetidin-3-amineHCID 10336591—
反応物1-(6-Amino-3,5-difluoropyridin-2-yl)-8-bromo-6,7-difluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acidHCID 15486977—
溶媒Dimethyl SulfoxideHCID 679—
生成物1-(6-Amino-3,5-difluoropyridin-2-yl)-8-bromo-7-(3-ethylaminoazetidin-1-yl)-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acidHCID 995804977.6%

反応条件

温度40 °C

反応手順

3-Ethylaminoazetidine (700 mg), 1-(6-amino-3,5-difluoropyridin-2-yl)-8-bromo-6,7-difluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (1.5 g), N-methyl-pyrrolidine (2.0 g)and dimethylsulfoxide (4.5 g) were combined, and the mixture was heated under stirring at 40° C. for 24 hours. After the mixture was allowed to cool down, isopropyl ether (10 mL) was added, the mixture was stirred, and a clear layer at the top of the mixture was removed. The same procedure was repeated once more, and the residue was concentrated under reduced pressure. Ethanol (5 mL) was added, and the mixture was heated under stirring at 70° C. for 30 minutes. The precipitated solid was collected by filtration. The title compound (1.38 g) was obtained.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US06858625B1
出典データセットuspto-grants-2005_02
ORD IDord-f1b6525d2c034223888dbf7e1495eaa4
出典メモuspto-grants-2005_02