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

HRID 33741노트

반응식

HRID 33741 반응식
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

참가 물질

5

반응물 3

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

생성물 1

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

시약·촉매·용매 1

HCID 962Water용매

실험 절차

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.

후처리

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

출처 및 근거

ORD 기록
ord-df20d167a6e64b09915674ff99213fbc
출처 데이터셋
uspto-grants-2008_09
특허 번호
US07429661B2

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