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HRID 1415938作成日:2026年10月25日

Dimethylformamide → 1-(3-amino-4,6-difluorophenyl)-7-[(3S)-3-aminopyrrolidin-1-yl]-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid

https://huagongshe.com/reaction/1415938

反応式

関与物質

役割名称HCID仕込み量
反応物DimethylformamideHCID 6228—
反応物TriethylamineHCID 8471—
反応物(3S)-(-)-3-AminopyrrolidineHCID 1519351—
反応物1-(3-Amino-4,6-difluorophenyl)-7-chloro-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acidHCID 11089970—
溶媒EthanolHCID 702—
生成物Diisopropyl EtherHCID 7914—
生成物1-(3-amino-4,6-difluorophenyl)-7-[(3S)-3-aminopyrrolidin-1-yl]-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acidHCID 11037172191.2%

反応条件

温度90 °C

反応手順

To 6,500 mg of N,N-dimethylformamide were added 1,300 mg of 1-(3-amino-4,6-difluorophenyl)-7-chloro-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid, 600 mg of (3S)-3-aminopyrrolidine, and 1,000 mg of triethylamine. The solution was stirred at 90° C. for 1 hour. The reaction solution was allowed to cool down, combined with 25 ml of ethanol, heated at reflux for 5 minutes, and allowed to cool down. The precipitate was collected by filtration and washed with ethanol and then with diisopropyl ether to give 1,410 mg of the title compound.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US05910498
出典データセットuspto-grants-1999_06
ORD IDord-b023eee62d134e96bb708fa16541416f
出典メモuspto-grants-1999_06