N-(4-(1-(4-methoxybenzyl)-1H-pyrazol-4-yl)-5-(piperidin-1-yl)thiazol-2-yl)pyridin-2-amine → 5-(piperidin-1-yl)-4-(1H-pyrazol-4-yl)-N-(pyridin-2-yl)thiazol-2-amine
反応式
COC1C=CC(C[N:8]2[CH:12]=[C:11]([C:13]3[N:14]=[C:15]([NH:24][C:25]4[CH:30]=[CH:29][CH:28]=[CH:27][N:26]=4)[S:16][C:17]=3[N:18]3[CH2:23][CH2:22][CH2:21][CH2:20][CH2:19]3)[CH:10]=[N:9]2)=CC=1>C(O)(C(F)(F)F)=O>[N:18]1([C:17]2[S:16][C:15]([NH:24][C:25]3[CH:30]=[CH:29][CH:28]=[CH:27][N:26]=3)=[N:14][C:13]=2[C:11]2[CH:10]=[N:9][NH:8][CH:12]=2)[CH2:19][CH2:20][CH2:21][CH2:22][CH2:23]1参加物
3
実験手順
According to Scheme 5 Step 3: A solution N-(4-(1-(4-methoxybenzyl)-1H-pyrazol-4-yl)-5-(piperidin-1-yl)thiazol-2-yl)pyridin-2-amine (0.58 mmol, 260 mg) in TFA (4 mL) was microwaved for 8 minutes at 140° C. After evaporation of the solvent, the crude residue was neutralized with a solution of NaOH (1 M). The aqueous phase was extracted with DCM. The organic phase was dried over MgSO4, was filtered and was concentrated to yield 5-(piperidin-1-yl)-4-(1H-pyrazol-4-yl)-N-(pyridin-2-yl)thiazol-2-amine (0.60 mmol, 195 mg, 99%) as a pale yellow solid.