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

HRID 369227노트

반응식

HRID 369227 반응식
[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

참가 물질

4

반응물 2

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

생성물 1

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

시약·촉매·용매 1

HCID 6228Dimethylformamide용매

반응 조건

온도
60 °C

실험 절차

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.

후처리

  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

출처 및 근거

ORD 기록
ord-3eed61f86d2e4e31b0fbff88bf5772a5
출처 데이터셋
uspto-grants-2000_10
특허 번호
US06136823

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