Triethylamine → N-{3-[1-(4-Cyano-3-fluoro-phenyl)-1-(3-methyl-3H-imidazol-4-yl)-ethylamino]-propyl}-3-hydroxy-benzenesulfonamide

HRID 1060896노트

반응식

HRID 1060896 반응식
Br[CH2:2][CH2:3][CH2:4][NH:5][S:6]([C:9]1[CH:14]=[CH:13][CH:12]=[C:11]([OH:15])[CH:10]=1)(=[O:8])=[O:7].[NH2:16][C:17]([C:25]1[CH:32]=[CH:31][C:28]([C:29]#[N:30])=[C:27]([F:33])[CH:26]=1)([C:19]1[N:20]([CH3:24])[CH:21]=[N:22][CH:23]=1)[CH3:18].CCN(CC)CC>CC#N>[C:29]([C:28]1[CH:31]=[CH:32][C:25]([C:17]([NH:16][CH2:2][CH2:3][CH2:4][NH:5][S:6]([C:9]2[CH:14]=[CH:13][CH:12]=[C:11]([OH:15])[CH:10]=2)(=[O:8])=[O:7])([C:19]2[N:20]([CH3:24])[CH:21]=[N:22][CH:23]=2)[CH3:18])=[CH:26][C:27]=1[F:33])#[N:30]

참가 물질

5

반응물 3

HCID 8471TriethylamineHCID 11470581(+)-4-[1-amino-1-(3-methyl-3H-imidazol-4-yl)-ethyl]-2-fluoro-benzonitrileHCID 18629458N-(3-bromo-propyl)-3-hydroxy-benzenesulfonamide

생성물 1

HCID 70026827N-{3-[1-(4-Cyano-3-fluoro-phenyl)-1-(3-methyl-3H-imidazol-4-yl)-ethylamino]-propyl}-3-hydroxy-benzenesulfonamide

시약·촉매·용매 1

HCID 6342Acetonitrile용매

실험 절차

N-(3-Bromo-propyl)-3-hydroxy-benzenesulfonamide (0.23 g, 0.782 mmol), (+)-4-[1-amino-1-(3-methyl-3H-imidazol-4-yl)-ethyl]-2-fluoro-benzonitrile (Example 1, Step I) (0.191 g, 0.78 mmol), and Et3N (0.218 mL, 1.56 mmol) were dissolved in CH3CN (5 mL) and heated at reflux for 16 h. The reaction mixture was concentrated in vacuo, azeotroped with toluene, and dried to give the title compound. MS (M+1) 458.

후처리

  1. temperatureheated
  2. temperatureat reflux for 16 h
  3. concentrationThe reaction mixture was concentrated in vacuo
  4. customazeotroped with toluene
  5. customdried

출처 및 근거

ORD 기록
ord-57d6f351b74f419ca0157b8ec036bd8f
출처 데이터셋
uspto-grants-2003_02
특허 번호
US06525074B2

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