Hydrochloric Acid → 1-(5-Amino-2,4-difluorophenyl)-8-chloro-6-fluoro-7-(2-hydroxy-1-methylethylamino)-4-oxo-1,4-dihydroquinoline-3-carboxylic Acid

HRID 369276ノート

反応式

HRID 369276 の反応式
[NH2:1][C:2]1[C:3]([F:26])=[CH:4][C:5]([F:25])=[C:6]([N:8]2[C:17]3[C:12](=[CH:13][C:14]([F:20])=[C:15](F)[C:16]=3[Cl:18])[C:11](=[O:21])[C:10]([C:22]([OH:24])=[O:23])=[CH:9]2)[CH:7]=1.[NH2:27][CH:28]([CH3:31])[CH2:29][OH:30].Cl>N1C=CC=CC=1>[NH2:1][C:2]1[C:3]([F:26])=[CH:4][C:5]([F:25])=[C:6]([N:8]2[C:17]3[C:12](=[CH:13][C:14]([F:20])=[C:15]([NH:27][CH:28]([CH3:31])[CH2:29][OH:30])[C:16]=3[Cl:18])[C:11](=[O:21])[C:10]([C:22]([OH:24])=[O:23])=[CH:9]2)[CH:7]=1

参加物

5

反応物 3

HCID 313Hydrochloric AcidHCID 51262-AminopropanolHCID 108619991-(3-Amino-4,6-difluorophenyl)-8-chloro-6,7-difluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid

生成物 1

HCID 232847051-(5-Amino-2,4-difluorophenyl)-8-chloro-6-fluoro-7-(2-hydroxy-1-methylethylamino)-4-oxo-1,4-dihydroquinoline-3-carboxylic Acid収率 73.1%

試薬・触媒・溶媒 1

HCID 1049Pyridine溶媒

反応条件

温度
50 °C

実験手順

1-(5-Amino-2,4-difluorophenyl)-8-chloro-6,7-difluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (200 mg) and 2-amino-1-propanol (200 mg) were added to pyridine (700 mg), and the mixture was stirred at 50° C. for 1.5 hours. Concentrated hydrochloric acid (200 mg) was added to the reaction mixture, and the resultant mixture was concentrated under reduced pressure. Ethanol (3 ml) was added to the residue, and deposits were collected by filtration and washed with ethanol and disopropyl ether in that order to obtain the title compound (167 mg) as a yellow powder.

後処理

  1. concentrationthe resultant mixture was concentrated under reduced pressure
  2. additionEthanol (3 ml) was added to the residue, and deposits
  3. filtrationwere collected by filtration
  4. washwashed with ethanol and disopropyl ether in that order

出典と根拠

ORDレコード
ord-e8b46cfcac8a49878c072d717252cf16
出典データセット
uspto-grants-2000_10
特許番号
US06136823

反応ノート

読み込み中…