Bis-(1H-imidazol-2-YL)-methanone → N-((3-(3-Fluoro-4-(4-morpholinyl)phenyl)-2-oxo-5-oxazolidinyl)methyl)phthalimide, (S)-

HRID 33742ノート

反応式

HRID 33742 の反応式
[C:1]1(=[O:29])[N:5]([CH2:6][C@H:7]([OH:23])[CH2:8][NH:9][C:10]2[CH:15]=[CH:14][C:13]([N:16]3[CH2:21][CH2:20][O:19][CH2:18][CH2:17]3)=[C:12]([F:22])[CH:11]=2)[C:4](=[O:24])[C:3]2=[CH:25][CH:26]=[CH:27][CH:28]=[C:2]12.[C:30](C1NC=CN=1)(C1NC=CN=1)=[O:31]>C(Cl)Cl>[F:22][C:12]1[CH:11]=[C:10]([N:9]2[CH2:8][C@H:7]([CH2:6][N:5]3[C:4](=[O:24])[C:3]4=[CH:25][CH:26]=[CH:27][CH:28]=[C:2]4[C:1]3=[O:29])[O:23][C:30]2=[O:31])[CH:15]=[CH:14][C:13]=1[N:16]1[CH2:17][CH2:18][O:19][CH2:20][CH2:21]1

参加物

4

反応物 2

HCID 5250894Bis-(1H-imidazol-2-YL)-methanoneHCID 16655949(R)-2-(3-((3-Fluoro-4-morpholinophenyl)amino)-2-hydroxypropyl)isoindoline-1,3-dione

生成物 1

HCID 12973056N-((3-(3-Fluoro-4-(4-morpholinyl)phenyl)-2-oxo-5-oxazolidinyl)methyl)phthalimide, (S)-収率 79.1%

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

N-[3-pthalimido-2-(R)-hydroxypropyl]-3-fluoro-4-(morpholinyl)aniline (57 gm) is dissolved in methylene dichloride (600 ml), carbonyl diimidazole (32 gm) is added at ambient temperature and the reaction mixture is stirred for 20 hours. The reaction mass is washed with water and methylene dichloride is distilled to give 48 gm of (S)-N-[[3-[3-Fluoro-4-[4-morpholinyl]phenyl]-2-oxo-5-oxazolidinyl]methyl]phthalimide as solid.

後処理

  1. washThe reaction mass is washed with water and methylene dichloride
  2. distillationis distilled

出典と根拠

ORDレコード
ord-2b95dc978d5f42ef9304f078b3507e96
出典データセット
uspto-grants-2008_09
特許番号
US07429661B2

反応ノート

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