반응식
C(N)C1C=CC=CC=1.[CH:9]1([CH2:12][CH2:13][NH2:14])[CH2:11][CH2:10]1.[CH3:15][C:16]1[N:17]=[C:18]([N:24]2[CH2:28][CH2:27][N:26]([CH2:29][C:30]3[CH:35]=[CH:34][C:33]([O:36][C:37]([F:40])([F:39])[F:38])=[CH:32][CH:31]=3)[C:25]2=[O:41])[S:19][C:20]=1[C:21](O)=[O:22]>>[CH:9]1([CH2:12][CH2:13][NH:14][C:21]([C:20]2[S:19][C:18]([N:24]3[CH2:28][CH2:27][N:26]([CH2:29][C:30]4[CH:31]=[CH:32][C:33]([O:36][C:37]([F:38])([F:39])[F:40])=[CH:34][CH:35]=4)[C:25]3=[O:41])=[N:17][C:16]=2[CH3:15])=[O:22])[CH2:11][CH2:10]1참가 물질
4
반응물 3
생성물 1
실험 절차
Following the procedure as describe in Example 8, making variations as required to replace benzylamine with 2-cyclopropylethylamine to react with 4-methyl-2-(2-oxo-3-(4-(trifluoromethoxy)benzyl)imidazolidin-1-yl)thiazole-5-carboxylic acid, the title compound was obtained as a white powder in 26% yield: mp 195-196° C. (ethyl acetate/hexanes); 1H NMR (300 MHz, CDCl3) δ 7.32 (d, J=8.4 Hz, 2H), 7.18 (d, J=8.4 Hz, 2H), 5.76 (s, 1H), 4.47 (s, 2H), 4.12-4.07 (m, 2H), 3.49-3.42 (m, 4H), 2.59 (s, 3H), 1.50-1.43 (m, 2H), 0.72-0.62 (m, 1H), 0.47-0.41 (m, 2H), 0.14-0.02 (m, 2H); 13C NMR (75 MHz, CDCl3) δ 162.3, 157.1, 155.4, 152.0, 148.9, 134.3, 129.7, 121.4, 120.4, 118.0, 47.3, 42.1, 41.8, 40.2, 34.3, 17.0, 8.6, 4.1; MS (ES+) m/z 469.3 (M+1).
출처 및 근거
- ORD 기록
- ord-315a11d2eff54c569d5f3aff31d69014
- 출처 데이터셋
- uspto-grants-2011_11
- 특허 번호
- US08063084B2
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