반응식
[NH2:1][C:2]1[C:7]2[C:8]([C:11]3[CH:16]=[CH:15][C:14]([NH:17][C:18]([C:20]4[N:21]([CH3:29])[C:22]5[C:27]([CH:28]=4)=[CH:26][CH:25]=[CH:24][CH:23]=5)=[O:19])=[C:13]([O:30][CH3:31])[CH:12]=3)=[CH:9][S:10][C:6]=2[C:5]([CH:32]2[CH2:34][CH:33]2[C:35]([O:37]CC)=[O:36])=[CH:4][N:3]=1.[OH-].[Na+].Cl>CO>[NH2:1][C:2]1[C:7]2[C:8]([C:11]3[CH:16]=[CH:15][C:14]([NH:17][C:18]([C:20]4[N:21]([CH3:29])[C:22]5[C:27]([CH:28]=4)=[CH:26][CH:25]=[CH:24][CH:23]=5)=[O:19])=[C:13]([O:30][CH3:31])[CH:12]=3)=[CH:9][S:10][C:6]=2[C:5]([CH:32]2[CH2:34][CH:33]2[C:35]([OH:37])=[O:36])=[CH:4][N:3]=1참가 물질
반응물 3
생성물 1
시약·촉매·용매 1
실험 절차
Ethyl 2-[4-amino-3-(3-methoxy-4-{[(1-methyl-1H-indol-2-yl)carbonyl]amino}phenyl)thieno[3,2-c]pyridin-7-yl]cyclopropanecarboxylate (433 mg, 0.8018 mmol) in methanol (2 mL) and 2M sodium hydroxide (1.604 mL, 3.207 mmol) was stirred for 23 hours at 50° C., cooled to room temperature and acidified to a pH of 4 with 1M hydrochloric acid. Solids were filtered off and washed with water. The material was purified by HPLC preparative to furnish the title compound as a white solid (61 mg 0.119 mmol): LCMS (Conditions a): MH30 =513 Rt=2.22 minutes; 1H NMR (DMSO-d6, 400 MHz) 9.51 (1 H), 7.99 (1 H), 7.71 (2 H), 7.57 (2 H), 7.34 (2 H), 7.19 (1 H), 7.15 (1 H), 7.07 (1 H), 5.46 (1 H), 4.04 (3 H), 3.91 (3 H), 2.39 (1 H), 1.73 (1 H), 1.46 (1 H), 1.39 (1 H).
후처리
- filtrationSolids were filtered off
- washwashed with water
- customThe material was purified by HPLC preparative
출처 및 근거
- ORD 기록
- ord-0a7089297df04bbb97bab492030c82dd
- 출처 데이터셋
- uspto-grants-2010_06
- 특허 번호
- US07737160B2
연결된 노트
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