Diisopropylethylamine → HCID 178522412、化合物

反応式

[Cl:1][C:2]1[CH:3]=[CH:4][C:5]([O:14][CH:15]2[CH2:17][CH2:16]2)=[C:6]([C:8]2[C:12]([NH2:13])=[CH:11][NH:10][N:9]=2)[CH:7]=1.[N:18]1[N:22]2[CH:23]=[CH:24][CH:25]=[N:26][C:21]2=[C:20]([C:27](Cl)=[O:28])[CH:19]=1.CCN(C(C)C)C(C)C>C1COCC1>[Cl:1][C:2]1[CH:3]=[CH:4][C:5]([O:14][CH:15]2[CH2:17][CH2:16]2)=[C:6]([C:8]2[C:12]([NH:13][C:27]([C:20]3[CH:19]=[N:18][N:22]4[CH:23]=[CH:24][CH:25]=[N:26][C:21]=34)=[O:28])=[CH:11][NH:10][N:9]=2)[CH:7]=1

参加物

実験手順

3-(5-chloro-2-cyclopropoxyphenyl)-1H-pyrazol-4-amine (0.2 g, 0.8 mmol) was dissolved in 15 mL of anhydrous THF. Pyrazolo[1,5-a]pyrimidine-3-carbonyl chloride (0.17 g, 0.96 mmol) was added followed by DIPEA (0.2 g, 1.6 mmol). The mixture was stirred at room temperature for 2 h, then evaporated to dryness. The residue was purified by silica gel chromatography (EtOAc as eluant) to afford 0.3 g of the title compound. Yield: 95%. 1H NMR (DMSO-d6, 400 MHz) δ: 12.93 (d, 1H), 9.56 (d, J=5.2 Hz, 1H), 9.34 (d, J=7.2 Hz, 1H), 8.75-8.74 (m, 1H), 8.65 (s, 1H), 8.22 (s, 0.5H), 8.05 (s, 0.5H), 7.55-7.25 (m, 4H), 3.97-3.94 (m, 1H), 0.70-0.44 (m, 4H).