1,2-Dichloroethane → (3S)-N-[4-(1-methyl-4,5-dihydro-1H-imidazol-2-yl)phenyl]-2N-(4-chlorophenylaminocarbonyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline-3-carboxamide

HRID 1432547노트

반응식

HRID 1432547 반응식
[Cl:1][C:2]1[CH:7]=[CH:6][C:5]([NH:8][C:9]([N:11]2[C@H:20]([C:21]([OH:23])=O)[CH2:19][C:18]3[C:13](=[CH:14][C:15]([O:26][CH3:27])=[C:16]([O:24][CH3:25])[CH:17]=3)[CH2:12]2)=[O:10])=[CH:4][CH:3]=1.[CH3:28][N:29]1[CH2:33][CH2:32][N:31]=[C:30]1[C:34]1[CH:39]=[CH:38][C:37]([NH2:40])=[CH:36][CH:35]=1.C(Cl)CCl>CN(C=O)C.O>[CH3:28][N:29]1[CH2:33][CH2:32][N:31]=[C:30]1[C:34]1[CH:39]=[CH:38][C:37]([NH:40][C:21]([C@@H:20]2[CH2:19][C:18]3[C:13](=[CH:14][C:15]([O:26][CH3:27])=[C:16]([O:24][CH3:25])[CH:17]=3)[CH2:12][N:11]2[C:9]([NH:8][C:5]2[CH:4]=[CH:3][C:2]([Cl:1])=[CH:7][CH:6]=2)=[O:10])=[O:23])=[CH:36][CH:35]=1

참가 물질

6

반응물 3

HCID 111,2-DichloroethaneHCID 227288764-(1-Methyl-4,5-dihydro-1H-imidazol-2-yl)-phenylamineHCID 86606520(3S)-2N-(4-chlorophenylaminocarbonyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid

생성물 1

HCID 11555757(3S)-N-[4-(1-methyl-4,5-dihydro-1H-imidazol-2-yl)phenyl]-2N-(4-chlorophenylaminocarbonyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline-3-carboxamide수율 57%

시약·촉매·용매 2

HCID 962Water용매HCID 6228Dimethylformamide용매

실험 절차

To a solution of (3S)-2N-(4-chlorophenylaminocarbonyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (25 mg, 0.064 mmol) and 4-(1-Methyl-4,5-dihydro-1H-imidazol-2-yl)-phenylamine (23 mg, 0.13 mmol) in DMF (2 mL) and H2O (0.5 mL) at room temperature, EDC (49 mg, 0.26 mmol) was added. The mixture was stirred at room for 2 h. It was concentrated in vacuo. The residue was purified by HPLC to give the titled compound as a white powder (20 mg). MS 548.2 and 550.2 (M+H, Cl pattern).

후처리

  1. concentrationIt was concentrated in vacuo
  2. customThe residue was purified by HPLC

출처 및 근거

ORD 기록
ord-abd7670ce7cd4e1583f650f3a1f079fd
출처 데이터셋
uspto-grants-2009_11
특허 번호
US07612089B2

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