Trifluoroacetic acid → 3-(2,7-diazaspiro[3.5]non-2-ylmethyl)-4-methoxy-6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridine
反応式
[CH3:1][O:2][C:3]1[C:4]2[N:5]([N:15]=[CH:16][C:17]=2[CH2:18][N:19]2[CH2:22][C:21]3([CH2:27][CH2:26][N:25](C(OC(C)(C)C)=O)[CH2:24][CH2:23]3)[CH2:20]2)[CH:6]=[C:7]([C:9]2[CH:10]=[N:11][N:12]([CH3:14])[CH:13]=2)[CH:8]=1.FC(F)(F)C(O)=O>ClCCl>[CH2:20]1[C:21]2([CH2:27][CH2:26][NH:25][CH2:24][CH2:23]2)[CH2:22][N:19]1[CH2:18][C:17]1[CH:16]=[N:15][N:5]2[CH:6]=[C:7]([C:9]3[CH:10]=[N:11][N:12]([CH3:14])[CH:13]=3)[CH:8]=[C:3]([O:2][CH3:1])[C:4]=12参加物
4
反応物 2
生成物 1
試薬・触媒・溶媒 1
実験手順
To a solution of tert-butyl 2-{[4-methoxy-6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridin-3-yl]methyl}-2,7-diazaspiro[3.5]nonane-7-carboxylate (47 mg, 0.10 mmol) in dichloromethane (2 ml) was added trifluoroacetic acid (0.008 mL, 0.1 mmol). After 30 minutes, the reaction mixture was concentrated. The residue was dissolved in methanol and eluted through a bicarbonate resin cartridge (StratoSpheres SPE, PL-HCO3 MP SPE) to give 3-(2,7-diazaspiro[3.5]non-2-ylmethyl)-4-methoxy-6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridine as a solid. 1H NMR (500 MHz, DMSO-d6) δ 8.51 (s, 1H); 8.24 (s, 1H); 7.97 (s, 1H); 7.12 (s, 1H); 6.77 (s, 1H); 3.95 (s, 3H); 3.85 (s, 3H); 3.79 (s, 2H); 2.89 (s, 4H); 2.50-2.54 (m, 4H); 1.47-1.50 (m, 4H). LRMS (ESI) calculated for C20H27N6O [M+H]+, 367.3; found 367.1.