反应详情

1.5 g (≅1.8 mmol) PS carbodiimide was added to a solution of 146 mg (0.93 mmol) N1-methyl-N1-(thiazol-5-yl)ethane-1,2-diamine and 252 mg (1.39 mmol) 3-(3-chlorophenyl)propiolic acid in DCM (10 ml) and the reaction solution was shaken for 16 h at RT. The resin was subsequently filtered off, washed with DCM and ethanol and the filtrate concentrated in a vacuum. CC (DCE/EtOH 10:1) was performed with the residue, whereby 63 mg (0.20 mmol, 21%) 3-(3-chlorophenyl)-N-(2-(methyl(thiazol-5-yl)amino)ethyl)propiolamide was obtained.

1. filtrationThe resin was subsequently filtered off
2. washwashed with DCM and ethanol
3. concentrationthe filtrate concentrated in a vacuum