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

HRID 369227ノート

反応式

HRID 369227 の反応式
[CH:1]1([NH2:4])[CH2:3][CH2:2]1.[NH2:5][C:6]1[C:7]([F:30])=[CH:8][C:9]([F:29])=[C:10]([N:12]2[C:21]3[C:16](=[CH:17][C:18]([F:24])=[C:19](F)[C:20]=3[Cl:22])[C:15](=[O:25])[C:14]([C:26]([OH:28])=[O:27])=[CH:13]2)[CH:11]=1>CN(C)C=O>[NH2:5][C:6]1[C:7]([F:30])=[CH:8][C:9]([F:29])=[C:10]([N:12]2[C:21]3[C:16](=[CH:17][C:18]([F:24])=[C:19]([NH:4][CH:1]4[CH2:3][CH2:2]4)[C:20]=3[Cl:22])[C:15](=[O:25])[C:14]([C:26]([OH:28])=[O:27])=[CH:13]2)[CH:11]=1

参加物

4

反応物 2

HCID 69828CyclopropylamineHCID 108619991-(3-Amino-4,6-difluorophenyl)-8-chloro-6,7-difluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid

生成物 1

HCID 232847731-(5-Amino-2,4-difluorophenyl)-8-chloro-7-cyclopropylamino-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic Acid収率 48.7%

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

反応条件

温度
60 °C

実験手順

Cyclopropylamine (50 mg) and 1-(5-amino-2,4-difluorophenyl)-8-chloro-6,7-difluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (150 mg) were, added to N,N-dimethylformamide (2 ml), and the mixtures was stirred at 60° C. for 2 hours. After the reaction mixture was cooled back to room temperature, the solvent was, distilled off under reduced pressure. Ethanol was added to the residue, and solids deposited were collected by filtration to obtain the title compound (80 mg) as a pale yellow powder.

後処理

  1. temperatureAfter the reaction mixture was cooled back to room temperature
  2. distillationdistilled off under reduced pressure
  3. additionEthanol was added to the residue, and solids
  4. filtrationdeposited were collected by filtration

出典と根拠

ORDレコード
ord-3eed61f86d2e4e31b0fbff88bf5772a5
出典データセット
uspto-grants-2000_10
特許番号
US06136823

反応ノート

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