1-Cyclopropyl-6,7-difluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid → 1-Cyclopropyl-6-fluoro-7-[3-(trifluoromethyl)-1-piperazinyl]-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid

HRID 248541노트

반응식

HRID 248541 반응식
[F:1][C:2]([F:10])([F:9])[CH:3]1[CH2:8][NH:7][CH2:6][CH2:5][NH:4]1.[CH:11]1([N:14]2[C:23]3[C:18](=[CH:19][C:20]([F:25])=[C:21](F)[CH:22]=3)[C:17](=[O:26])[C:16]([C:27]([OH:29])=[O:28])=[CH:15]2)[CH2:13][CH2:12]1>N1C=CC=CC=1>[CH:11]1([N:14]2[C:23]3[C:18](=[CH:19][C:20]([F:25])=[C:21]([N:7]4[CH2:6][CH2:5][NH:4][CH:3]([C:2]([F:10])([F:9])[F:1])[CH2:8]4)[CH:22]=3)[C:17](=[O:26])[C:16]([C:27]([OH:29])=[O:28])=[CH:15]2)[CH2:12][CH2:13]1

참가 물질

4

반응물 2

HCID 52104221-Cyclopropyl-6,7-difluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acidHCID 185197252-(Trifluoromethyl)piperazine

생성물 1

HCID 197635981-Cyclopropyl-6-fluoro-7-[3-(trifluoromethyl)-1-piperazinyl]-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid

시약·촉매·용매 1

HCID 1049Pyridine용매

반응 조건

온도
77 °C

실험 절차

A 0.55 g portion of 2-(trifluoromethyl)piperazine was dissolved in 14 ml of pyridine. To this was added 265 mg of 1-cyclopropyl-6,7-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid. The mixture was stirred for 3 hours at 77° C.. The pyridine was removed by repeated evaporation with toluene. The residue was triturated with hot methanol. The resulting solid was collected, washed with methanol and ether and dried, giving 105 mg of the desired product as a colorless solid.

후처리

  1. customThe pyridine was removed
  2. customevaporation with toluene
  3. customThe residue was triturated with hot methanol
  4. customThe resulting solid was collected
  5. washwashed with methanol and ether
  6. customdried

출처 및 근거

ORD 기록
ord-bd8ffc8200004476b67fedaae80e53b4
출처 데이터셋
uspto-grants-1993_05
특허 번호
US05210193

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