5-Fluoro-2-(trifluoromethyl)benzoyl chloride → 6-[4-(5-FLUORO-2-TRIFLUOROMETHYLBENZOYL)PIPERAZIN-1-YL]PYRIDAZINE-3-CARBOXYLIC Acid (4-METHYLPENTYL)AMIDE
反応式
[F:1][C:2]1[CH:3]=[CH:4][C:5]([C:11]([F:14])([F:13])[F:12])=[C:6]([CH:10]=1)[C:7](Cl)=[O:8].[CH3:15][CH:16]([CH3:35])[CH2:17][CH2:18][CH2:19][NH:20][C:21]([C:23]1[N:24]=[N:25][C:26]([N:29]2[CH2:34][CH2:33][NH:32][CH2:31][CH2:30]2)=[CH:27][CH:28]=1)=[O:22]>>[CH3:15][CH:16]([CH3:35])[CH2:17][CH2:18][CH2:19][NH:20][C:21]([C:23]1[N:24]=[N:25][C:26]([N:29]2[CH2:34][CH2:33][N:32]([C:7](=[O:8])[C:6]3[CH:10]=[C:2]([F:1])[CH:3]=[CH:4][C:5]=3[C:11]([F:14])([F:13])[F:12])[CH2:31][CH2:30]2)=[CH:27][CH:28]=1)=[O:22]参加物
3
実験手順
Following the procedure of Example 3, making variations only as required to use 5-fluoro-2-trifluoromethylbenzoyl chloride in place of isoxazole-5-carbonyl chloride to react with 6-piperazin-1-yl-pyridazine-3-carboxylic acid (4-methylpentyl)amide, the title compound was obtained as a white solid (10% yield). 1H NMR (300 MHz, CDCl3) δ 8.04, 7.86, 7.75-7.71, 7.26-7.22, 7.08-7.04, 6.98, 4.10-3.98, 3.90-3.70, 3.46-3.40, 3.36-3.33, 1.61-1.50, 1.28-1.20, 0.85. 13C NMR (75 MHz, CDCl3) 6166.0, 162.9, 162.6, 159.9, 145.5, 136.8, 129.7, 127.6, 127.7, 127.2, 125.1, 123.3, 121.4, 116.8, 116.5, 114.9, 114.6, 113.9, 112.5, 46.3, 44.5, 44.3, 41.3, 39.7, 36.0, 27.8, 27.4, 22.5. MS (ES+) m/z 482.4 (M+1).