Garenoxacin → HCID 68434103、化合物

HRID 1018540ノート

反応式

HRID 1018540 の反応式
[CH:1]1([N:4]2[C:13]3[C:8](=[CH:9][CH:10]=[C:11]([C:18]4[CH:19]=[C:20]5[C:24](=[CH:25][CH:26]=4)[C@@H:23]([CH3:27])[NH:22][CH2:21]5)[C:12]=3[O:14][CH:15]([F:17])[F:16])[C:7](=[O:28])[C:6]([C:29]([OH:31])=[O:30])=[CH:5]2)[CH2:3][CH2:2]1>C(O)(=O)C>[C:29]([OH:31])(=[O:30])[CH3:6].[CH:1]1([N:4]2[C:13]3[C:8](=[CH:9][CH:10]=[C:11]([C:18]4[CH:19]=[C:20]5[C:24](=[CH:25][CH:26]=4)[C@@H:23]([CH3:27])[NH:22][CH2:21]5)[C:12]=3[O:14][CH:15]([F:17])[F:16])[C:7](=[O:28])[C:6]([C:29]([OH:31])=[O:30])=[CH:5]2)[CH2:3][CH2:2]1

参加物

3

反応物 1

HCID 124093Garenoxacin

生成物 1

HCID 68434103HCID 68434103、化合物収率 84.1%

試薬・触媒・溶媒 1

HCID 176Acetic Acid溶媒

反応条件

温度
80 °C

実験手順

In 0.75 ml of acetic acid is suspended 0.5 g of (R)-1-cyclopropyl-8-difluoromethoxy-7-(1-methyl-2,3-dihydro-1H-5-isoindolyl)-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid and the suspension is warmed to 80° C. to form a uniform solution. Subsequently, the solution is filtered at the same temperature and then 2.5 ml of ethanol is added to the filtrate, after which the crystals deposited are collected by filtration to obtain 0.24 g of (R)-1-cyclopropyl-8-difluoromethoxy-7-(1-methyl-2,3-dihydro-1H-5-isoindolyl)-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid acetate.

後処理

  1. customto form a uniform solution
  2. filtrationSubsequently, the solution is filtered at the same temperature
  3. addition2.5 ml of ethanol is added to the filtrate
  4. filtrationafter which the crystals deposited are collected by filtration

出典と根拠

ORDレコード
ord-84d2945c7733483db950bd4275b19b34
出典データセット
uspto-grants-2002_11
特許番号
US06482835B2

反応ノート

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