7-[2-(3-chloro-pyridin-2-yl)-5-methoxy-2H-pyrazol-3-yl]-2-(4-methoxy-benzyl)-5-methyl-2H-8-oxa-1,2,6-triaza-cyclopenta[a]naphthalen-9-one → 6-{[2-(3-chloro-pyridin-2-yl)-5-methoxy-2H-pyrazole-3-carbonyl]-amino}-2-(4-methoxy-benzyl)-5-methyl-2H-indazole-7-carboxylic acid isopropyl amide
반응식
[Cl:1][C:2]1[C:3]([N:8]2[C:12]([C:13]3[O:22][C:21](=[O:23])[C:20]4[C:19]5=[N:24][N:25]([CH2:27][C:28]6[CH:33]=[CH:32][C:31]([O:34][CH3:35])=[CH:30][CH:29]=6)[CH:26]=[C:18]5[CH:17]=[C:16]([CH3:36])[C:15]=4[N:14]=3)=[CH:11][C:10]([O:37][CH3:38])=[N:9]2)=[N:4][CH:5]=[CH:6][CH:7]=1>O1CCCC1.C(N)(C)C>[CH:12]([NH:8][C:21]([C:20]1[C:19]2[C:18](=[CH:26][N:25]([CH2:27][C:28]3[CH:29]=[CH:30][C:31]([O:34][CH3:35])=[CH:32][CH:33]=3)[N:24]=2)[CH:17]=[C:16]([CH3:36])[C:15]=1[NH:14][C:13]([C:12]1[N:8]([C:3]2[C:2]([Cl:1])=[CH:7][CH:6]=[CH:5][N:4]=2)[N:9]=[C:10]([O:37][CH3:38])[CH:11]=1)=[O:22])=[O:23])([CH3:13])[CH3:11]참가 물질
4
반응물 1
생성물 1
시약·촉매·용매 2
반응 조건
- 온도
- 20 °C
실험 절차
A solution of 7-[2-(3-chloro-pyridin-2-yl)-5-methoxy-2H-pyrazol-3-yl]-2-(4-methoxy-benzyl)-5-methyl-2H-8-oxa-1,2,6-triaza-cyclopenta[a]naphthalen-9-one (0.100 g, 0.189 mmol) in tetrahydrofurane (2 ml) was treated with 16 drops of isopropyl amine and stirred at 20° C. for three hours. The reaction mixture was evaporated and the crude product was purified by flash chromatography on silica gel using a mixture of 75% ethyl acetate 25% cyclohexane. The desired product showed the physical data reported in the corresponding table (P.34.).
후처리
- customThe reaction mixture was evaporated
- customthe crude product was purified by flash chromatography on silica gel using
- additiona mixture of 75% ethyl acetate 25% cyclohexane
출처 및 근거
- ORD 기록
- ord-1f87041f4a054198808f8a7f123c1b28
- 출처 데이터셋
- uspto-grants-2013_12
- 특허 번호
- US08598078B2
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