Trifluoroacetic acid → HCID 67327163、化合物

反応式

FC(F)(F)C(O)=O.[C:8]([C:10]1[CH:15]=[CH:14][N:13]2[N:16]=[CH:17][C:18]([C:19]3[N:24]=[C:23]([NH:25][C@@H:26]4[CH2:31][CH2:30][CH2:29][N:28](C(OC(C)(C)C)=O)[CH2:27]4)[CH:22]=[CH:21][N:20]=3)=[C:12]2[CH:11]=1)#[N:9].C(=O)([O-])O.[Na+]>ClCCl>[NH:28]1[CH2:29][CH2:30][CH2:31][C@@H:26]([NH:25][C:23]2[CH:22]=[CH:21][N:20]=[C:19]([C:18]3[CH:17]=[N:16][N:13]4[CH:14]=[CH:15][C:10]([C:8]#[N:9])=[CH:11][C:12]=34)[N:24]=2)[CH2:27]1

参加物

実験手順

Trifluoroacetic acid (0.61 mL, 7.97 mmol) was added to a stirred solution of (R)-tert-butyl 3-(2-(5-cyanopyrazolo[1,5-a]pyridin-3-yl)pyrimidin-4-ylamino)piperidine-1-carboxylate (Preparation 7a, 0.12 g, 0.27 mmol) in dichloromethane (4 mL) and the mixture was stirred at room temperature for 4 hours. 4% Aqueous sodium hydrogencarbonate solution and solid sodium hydrogencarbonate were then added until the pH was basic and the mixture was further extracted with more dichloromethane. The organic layer was separated, dried (MgSO4) and evaporated to give the title compound (0.06 g, 62%) as a pale yellow solid which was used in the next synthetic step without further purification.