Dimethylformamide → (R)-2-(3-((3-Fluoro-4-morpholinophenyl)amino)-2-hydroxypropyl)isoindoline-1,3-dione

HRID 33741ノート

反応式

HRID 33741 の反応式
Cl[CH2:2][C@H:3]([OH:19])[CH2:4][NH:5][C:6]1[CH:11]=[CH:10][C:9]([N:12]2[CH2:17][CH2:16][O:15][CH2:14][CH2:13]2)=[C:8]([F:18])[CH:7]=1.[C:20]1(=[O:30])[NH:24][C:23](=[O:25])[C:22]2=[CH:26][CH:27]=[CH:28][CH:29]=[C:21]12.[K].CN(C)C=O>O>[C:20]1(=[O:30])[N:24]([CH2:2][C@H:3]([OH:19])[CH2:4][NH:5][C:6]2[CH:11]=[CH:10][C:9]([N:12]3[CH2:17][CH2:16][O:15][CH2:14][CH2:13]3)=[C:8]([F:18])[CH:7]=2)[C:23](=[O:25])[C:22]2=[CH:26][CH:27]=[CH:28][CH:29]=[C:21]12

参加物

5

反応物 3

HCID 6228DimethylformamideHCID 16655948(2R)-1-Chloro-3-[[3-fluoro-4-(4-morpholinyl)phenyl]amino]-2-propanolHCID 24194345Phthalimide potassium salt

生成物 1

HCID 16655949(R)-2-(3-((3-Fluoro-4-morpholinophenyl)amino)-2-hydroxypropyl)isoindoline-1,3-dione

試薬・触媒・溶媒 1

HCID 962Water溶媒

実験手順

The mixture of (N-[3-Chloro-2-(R)-hydroxypropyl]-3-fluoro-4-morpholinyl aniline obtained in example 1, potassium phthalimide (40 gm) and Dimethyl formamide (400 ml) is heated for 5 hours at reflux temperature. The reaction mixture is cooled to ambient temperature, poured in to water (2 L) and filtered the solid obtained, and recrystallized from isopropyl alcohol to give 50 gm N-[3-pthalimido-2-(R)-hydroxypropyl]-3-fluoro-4-(morpholinyl)aniline.

後処理

  1. temperatureis heated for 5 hours
  2. temperatureat reflux temperature
  3. filtrationfiltered the solid
  4. customobtained
  5. customrecrystallized from isopropyl alcohol

出典と根拠

ORDレコード
ord-df20d167a6e64b09915674ff99213fbc
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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