반응식
[Cl:1][C:2]1[C:10]([O:11][CH2:12][CH2:13][CH2:14][O:15][Si:16]([C:19]([CH3:22])([CH3:21])[CH3:20])([CH3:18])[CH3:17])=[CH:9][C:8]([C:23]2[N:24]([C:34]([O:36][C:37]([CH3:40])([CH3:39])[CH3:38])=[O:35])[C:25]3[C:30]([CH:31]=2)=[CH:29][C:28]([CH:32]=O)=[CH:27][CH:26]=3)=[C:7]2[C:3]=1[CH2:4][NH:5][C:6]2=[O:41].[CH3:42][NH:43][CH3:44].C1COCC1.C(O)(=O)C.C(O[BH-](OC(=O)C)OC(=O)C)(=O)C.[Na+]>C(#N)C>[Cl:1][C:2]1[C:10]([O:11][CH2:12][CH2:13][CH2:14][O:15][Si:16]([C:19]([CH3:22])([CH3:21])[CH3:20])([CH3:17])[CH3:18])=[CH:9][C:8]([C:23]2[N:24]([C:34]([O:36][C:37]([CH3:39])([CH3:40])[CH3:38])=[O:35])[C:25]3[C:30]([CH:31]=2)=[CH:29][C:28]([CH2:32][N:43]([CH3:44])[CH3:42])=[CH:27][CH:26]=3)=[C:7]2[C:3]=1[CH2:4][NH:5][C:6]2=[O:41]참가 물질
6
반응물 4
생성물 1
시약·촉매·용매 1
실험 절차
In a similar manner to Step 2 of Example 6, 4-chloro-5-[3-(tert-butyldimethylsiloxy)propoxy]-7-[1-(tert-butoxycarbonyl)-5-formylindol-2-yl]isoindolinone (74.9 mg, 0.125 mmol) was dissolved in acetonitrile (2.5 mL), and the solution was treated with 2.0 mol/L dimethylamine-THF solution (0.63 mL, 1.25 mmol), acetic acid (0.072 mL, 1.25 mmol) and sodium triacetoxyborohydride (76.5 mg, 0.375 mmol), followed by purification by flash column chromatography (chloroform/methanol=19/1, 4/1) to obtain 4-chloro-5-[3-(tert-butyldimethylsiloxy)propyloxy]-7-[1-(tert-butoxycarbonyl)-5-(dimethylaminomethyl)indol-2-yl]isoindolinone (65.0 mg, yield 83%).
후처리
- customfollowed by purification by flash column chromatography (chloroform/methanol=19/1, 4/1)
출처 및 근거
- ORD 기록
- ord-2511e98e75604dafa94df0a2bce4c564
- 출처 데이터셋
- uspto-grants-2010_06
- 특허 번호
- US07745641B2
연결된 노트
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