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 248541ノート

反応式

HRID 248541 の反応式
[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

参加物

4

反応物 2

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

生成物 1

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

試薬・触媒・溶媒 1

HCID 1049Pyridine溶媒

反応条件

温度
77 °C

実験手順

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.

後処理

  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

出典と根拠

ORDレコード
ord-bd8ffc8200004476b67fedaae80e53b4
出典データセット
uspto-grants-1993_05
特許番号
US05210193

反応ノート

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