반응식
[CH2:1]([N:8]([CH:35]([CH3:37])[CH3:36])[C:9](=[O:34])[CH2:10][N:11]1[C:20](=[O:21])[CH2:19][C:18]2[N:14]([C:15]([C:22]3[CH:27]=[CH:26][CH:25]=[CH:24][CH:23]=3)=[N:16][N:17]=2)[C:13]2[CH:28]=[C:29]([F:33])[C:30]([F:32])=[CH:31][C:12]1=2)[C:2]1[CH:7]=[CH:6][CH:5]=[CH:4][CH:3]=1.[F:38][C:39]1[CH:47]=[C:46]2[C:42]([C:43]([CH:48]=O)=[CH:44][NH:45]2)=[CH:41][CH:40]=1>>[CH2:1]([N:8]([CH:35]([CH3:37])[CH3:36])[C:9](=[O:34])[CH2:10][N:11]1[C:20](=[O:21])[C:19](=[CH:48][C:43]2[C:42]3[C:46](=[CH:47][C:39]([F:38])=[CH:40][CH:41]=3)[NH:45][CH:44]=2)[C:18]2[N:14]([C:15]([C:22]3[CH:27]=[CH:26][CH:25]=[CH:24][CH:23]=3)=[N:16][N:17]=2)[C:13]2[CH:28]=[C:29]([F:33])[C:30]([F:32])=[CH:31][C:12]1=2)[C:2]1[CH:3]=[CH:4][CH:5]=[CH:6][CH:7]=1참가 물질
3
반응물 2
생성물 1
실험 절차
Following the procedure described for Example 1(A), Step A, N-benzyl-2-(8,9-difluoro-5-oxo-1-phenyl-4,5-dihydro-2,3,6,10b-tetraaza-benzo[e]azulen-6-yl)-N-isopropyl-acetamide (Preparation 9) (50 mg, 0.099 mmol) was condensed with 6-fluoroindole-3-carboxaldehyde (19.4 mg, 0.119 mmol). Purification by medium pressure chromatography eluting with 50% EtOAc in CH2Cl2 yielded 23.5 mg of N-benzyl-2-[8,9-difluoro-4-(6-fluoro-1H-indol-3-ylmethylene)-5-oxo-1-phenyl-4,5-dihydro-2,3,6,10b-tetraaza-benzo[e]azulen-6-yl]-N-isopropyl-acetamide. 1H NMR (CDCl3) δ 7.94 (d, 1H), 7.61 (m, 3H), 7.27-7.49 (m, 9H), 6.95 (m, 1H), 6.86 (m, 1H), 6.63 (m, 1H), 4.35-5.0 (m, 5H), 4.20 (m, 1H), 1.23 (m, 6H): MS 647.3 (M+1), 645.3 (M−1).
후처리
- customPurification by medium pressure chromatography
- washeluting with 50% EtOAc in CH2Cl2
출처 및 근거
- ORD 기록
- ord-535caa4ff3be487fb3c2c1297c381b76
- 출처 데이터셋
- uspto-grants-2008_04
- 특허 번호
- US07358242B2
연결된 노트
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