반응식
[F:1][C:2]1[CH:22]=[CH:21][C:5]([CH2:6][CH:7]2[C:16]3[C:11](=[CH:12][C:13]([O:19][CH3:20])=[C:14]([O:17][CH3:18])[CH:15]=3)[CH2:10][CH2:9][NH:8]2)=[CH:4][CH:3]=1.[C:23]([O:27][C:28](=[O:33])[NH:29][CH2:30][CH2:31]Br)([CH3:26])([CH3:25])[CH3:24].CCN(C(C)C)C(C)C>C1COCC1>[C:23]([O:27][C:28](=[O:33])[NH:29][CH2:30][CH2:31][N:8]1[CH2:9][CH2:10][C:11]2[C:16](=[CH:15][C:14]([O:17][CH3:18])=[C:13]([O:19][CH3:20])[CH:12]=2)[CH:7]1[CH2:6][C:5]1[CH:4]=[CH:3][C:2]([F:1])=[CH:22][CH:21]=1)([CH3:26])([CH3:25])[CH3:24]참가 물질
5
반응 조건
- 온도
- 70 °C
실험 절차
To a solution of 1-(4-fluorobenzyl)-6,7-dimethoxy-1,2,3,4-tetrahydro-isoquinoline (example A31, 1.05 g, 3.5 mmol) in THF (40 mL) is added (2-bromo-ethyl)-carbamic acid tert-butyl ester (example B1, 0.94 g, 4.2 mmol) and DIPEA. The reaction mixture is stirred at 70° C. in a sealed flask for 5 days. After cooling to rt, the reaction mixture is evaporated to dryness, and the residue is purified by preparative HPLC to provide the title compound.
후처리
- temperatureAfter cooling to rt
- customthe reaction mixture is evaporated to dryness
- customthe residue is purified by preparative HPLC
출처 및 근거
- ORD 기록
- ord-cf33ce8e019049ccb201b8713b078e9f
- 출처 데이터셋
- uspto-grants-2004_11
- 특허 번호
- US06815451B2
연결된 노트
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