Trifluoroacetic acid → (R)-N-(Piperidin-3-yl)-6-(pyrazolo[1,5-a]pyridin-3-yl)pyrazin-2-amine
反応式
FC(F)(F)C(O)=O.[N:8]1[N:12]2[CH:13]=[CH:14][CH:15]=[CH:16][C:11]2=[C:10]([C:17]2[N:22]=[C:21]([NH:23][C@@H:24]3[CH2:29][CH2:28][CH2:27][N:26](C(OC(C)(C)C)=O)[CH2:25]3)[CH:20]=[N:19][CH:18]=2)[CH:9]=1>C(Cl)Cl>[NH:26]1[CH2:27][CH2:28][CH2:29][C@@H:24]([NH:23][C:21]2[CH:20]=[N:19][CH:18]=[C:17]([C:10]3[CH:9]=[N:8][N:12]4[CH:13]=[CH:14][CH:15]=[CH:16][C:11]=34)[N:22]=2)[CH2:25]1参加物
4
実験手順
Trifluoroacetic acid (0.35 mL, 4.56 mmol) was added to a solution of (R)-tert-butyl 3-(6-(pyrazolo[1,5-a]pyridin-3-yl)pyrazin-2-ylamino)piperidine-1-carboxylate (Preparation 28a, 0.30 g, 0.76 mmol) in methylene chloride (10 mL) and the resulting solution was stirred at ambient temperature overnight and then at 50° C. for additional 24 h. The solvent was then evaporated and the residue was redissolved in methylene chloride and washed with a 10% aqueous sodium hydroxide solution. The organic phase was dried over magnesium sulphate, filtered and the solvent was evaporated. The crude product was purified by flash chromatography (10-15% MeOH/CH2Cl2/NH3) to yield the title compound (0.125 g, 56%) as an oil.