N-{5-[3-(2-Chloro-4-pyrimidinyl)pyrazolo[1,5-a]pyridin-2-yl]-2-methylphenyl}-2-(2-thienyl)acetamide → N-[3-(3-{2-[(7-Amino-5,6,7,8-tetrahydro-2-naphthalenyl)amino]-4-pyrimidinyl}pyrazolo[1,5-a]pyridin-2-yl)phenyl]-2-(2-thienyl)acetamide
반응식
Cl[C:2]1[N:7]=[C:6]([C:8]2[C:9]([C:17]3[CH:18]=[CH:19][C:20](C)=[C:21]([NH:23][C:24](=[O:31])[CH2:25][C:26]4[S:27][CH:28]=[CH:29][CH:30]=4)[CH:22]=3)=[N:10][N:11]3[CH:16]=[CH:15][CH:14]=[CH:13][C:12]=23)[CH:5]=[CH:4][N:3]=1.Cl.Cl.CN(C)CCO[C:40]1[CH:41]=[C:42]([CH:44]=[CH:45][CH:46]=1)[NH2:43]>>[NH2:7][CH:6]1[CH2:8][C:40]2[CH:41]=[C:42]([NH:43][C:2]3[N:7]=[C:6]([C:8]4[C:9]([C:17]5[CH:22]=[C:21]([NH:23][C:24](=[O:31])[CH2:25][C:26]6[S:27][CH:28]=[CH:29][CH:30]=6)[CH:20]=[CH:19][CH:18]=5)=[N:10][N:11]5[CH:16]=[CH:15][CH:14]=[CH:13][C:12]=45)[CH:5]=[CH:4][N:3]=3)[CH:44]=[CH:45][C:46]=2[CH2:4][CH2:5]1참가 물질
3
반응물 2
생성물 1
실험 절차
N-{5-[3-(2-chloro-4-pyrimidinyl)pyrazolo[1,5-a]pyridin-2-yl]-2-methylphenyl}-2-(2-thienyl)acetamide (100 mg, 0.22 mmol) and 3-{[2-(dimethylamino)ethyl]oxy}-aniline dihydrochloride (112 mg, 0.44 mmol) were coupled according to the procedure of Example 56, Step H to give 25 mg of the title compound (19%). 1H NMR (400 MHz, d6-DMSO) δ 9.63 (s, 1H), 9.53 (s, 1H), 8.81 (d, J=7.2 Hz, 1H), 8.49 (d, J=9.2 Hz, 1H), 8.23 (d, J=5.6 Hz, 1H), 7.72 (s, 1H), 7.52 (s, 1H), 7.47-7.43 (m, 1H), 7.36 (d, J=4.8 Hz, 1H), 7.30-7.25 (m, 3H), 7.14-7.08 (m, 2H), 6.97-6.95 (m, 2H), 6.52-6.50 (m, 2H), 3.97 (m, 2H), 3.90 (s, 2H), 2.58 (t, J=5.6 Hz, 2H), 2.26 (s, 3H), 2.17 (s, 6H) ppm. ES-LC/MS m/z=604 [M+H]+.
출처 및 근거
- ORD 기록
- ord-a4c3b4f2f6fc4d6fac5b00ddcc2c6f94
- 출처 데이터셋
- uspto-grants-2010_10
- 특허 번호
- US07807673B2
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