反应详情

A mixture of acid 1-6 (10.8 mg, 0.04 mmol), EDC (7.7 mg, 0.04 mmol), HOBT (5.4 mg, 0.04 mmol) and NMM (0.026 mL, 0.24 mmol) in DMF (1 mL) was agitated until clear solution. After 30 minutes, amine 12-1 was added. The solution was agitated for one minute and then let stand for 18 h. The solution was diluted with ethyl acetate, washed with sat. NaHCO3 and H2O. Following evaporative removal of the solvent, the residue was dissolved in 90:10 TFA/H2O (1 ml). After 2 h, the solvents were evaporated to give acid 12-2.

1. stirringThe solution was agitated for one minute
2. waitlet stand for 18 h
3. washwashed with sat. NaHCO3 and H2O
4. customremoval of the solvent
5. dissolutionthe residue was dissolved in 90:10 TFA/H2O (1 ml)
6. waitAfter 2 h
7. customthe solvents were evaporated