反应详情

2-Aminothiazole-4-carboxylate hydrobromide salt (Chempacific; 1.13 g, 5.02 mmol), HATU (2.87 g, 7.53 mmol) and 4-amino-1-methylpiperidine (0.86 g, 7.53 mmol) were stirred in DMF (5 mL) and DIPEA (5.2 mL, 30.12 mmol) added. The mixture was stirred at room temperature overnight. The reaction mixture was concentrated and the residue taken up in methanol, absorbed onto an SCX column, washed with methanol and eluted with ammonia in methanol. Product containing fractions were combined, evaporated and the residue and further purified by column chromatography (5% 7N NH3 in MeOH/DCM) Product containing fractions were combined and evaporated to give the title compound as a yellow solid (635 mg, 53%).

1. concentrationThe reaction mixture was concentrated
2. customabsorbed onto an SCX column
3. washwashed with methanol
4. washeluted with ammonia in methanol
5. additionProduct containing fractions
6. customevaporated
7. customthe residue and further purified by column chromatography (5% 7N NH3 in MeOH/DCM) Product
8. additioncontaining fractions
9. customevaporated