Methyl(2-(morpholin-4-yl)ethyl)amine → 4-[4-{2-[bis-(4-methoxy-benzyl)-amino]-pyrimidin-5-yl}-2-morpholin-4-yl-5,6-dihydro-pyrrolo[2,3-d]pyrimidin-7-yl]-N-methyl-N-(2-morpholin-4-yl-ethyl)-benzamide
반응식
[CH3:1][NH:2][CH2:3][CH2:4][N:5]1[CH2:10][CH2:9][O:8][CH2:7][CH2:6]1.[CH3:11][O:12][C:13]1[CH:59]=[CH:58][C:16]([CH2:17][N:18]([CH2:49][C:50]2[CH:55]=[CH:54][C:53]([O:56][CH3:57])=[CH:52][CH:51]=2)[C:19]2[N:24]=[CH:23][C:22]([C:25]3[C:26]4[CH2:39][CH2:38][N:37]([C:40]5[CH:48]=[CH:47][C:43]([C:44]([OH:46])=O)=[CH:42][CH:41]=5)[C:27]=4[N:28]=[C:29]([N:31]4[CH2:36][CH2:35][O:34][CH2:33][CH2:32]4)[N:30]=3)=[CH:21][N:20]=2)=[CH:15][CH:14]=1>>[CH3:57][O:56][C:53]1[CH:54]=[CH:55][C:50]([CH2:49][N:18]([CH2:17][C:16]2[CH:15]=[CH:14][C:13]([O:12][CH3:11])=[CH:59][CH:58]=2)[C:19]2[N:20]=[CH:21][C:22]([C:25]3[C:26]4[CH2:39][CH2:38][N:37]([C:40]5[CH:48]=[CH:47][C:43]([C:44]([N:2]([CH3:1])[CH2:3][CH2:4][N:5]6[CH2:10][CH2:9][O:8][CH2:7][CH2:6]6)=[O:46])=[CH:42][CH:41]=5)[C:27]=4[N:28]=[C:29]([N:31]4[CH2:32][CH2:33][O:34][CH2:35][CH2:36]4)[N:30]=3)=[CH:23][N:24]=2)=[CH:51][CH:52]=1참가 물질
반응물 2
생성물 1
실험 절차
Using methyl-(2-morpholin-4-yl-ethyl)-amine (29.8 mg, 0.206 mmol) obtained in Step A instead of 3-(aminomethyl)pyridine, and 4-(4-{2-[bis-(4-methoxy-benzyl)-amino]-pyrimidin-5-yl}-2-morpholin-4-yl-5,6-dihydro-pyrrolo[2,3-d]pyrimidin-7-yl)-benzoic acid (68.1 mg, 0.103 mmol) obtained in Step A in Example 1-D-19, in the same manner as Step B in Example 1-D-19, amidation was carried out, to obtain a crude product of 4-[4-{2-[bis-(4-methoxy-benzyl)-amino]-pyrimidin-5-yl}-2-morpholin-4-yl-5,6-dihydro-pyrrolo[2,3-d]pyrimidin-7-yl]-N-methyl-N-(2-morpholin-4-yl-ethyl)-benzamide as a yellow solid (70.2 mg), and then the PMB groups were removed according to the above Deprotection method 3, to obtain the desired compound (D-139) as a yellow powder (42.0 mg, 75%).
출처 및 근거
- ORD 기록
- ord-0a0d6f53bfb94c6085468b56436d6da7
- 출처 데이터셋
- uspto-grants-2011_09
- 특허 번호
- US08022205B2
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