反应详情

685 μl (4.38 mmol) DIC was added to a solution of 785 mg (4.00 mmol) N-methyl-1-(thiazol-2-yl)piperidin-4-amine and 640 mg (4.38 mmol) 3-phenyl-propiolic acid in MeCN (40 ml) and the reaction solution was stirred for 3 h at RT. Subsequently, concentration took place in vacuo and the residue was taken up by chloroform, washed with water and brine, dried over MgSO4, filtered and concentrated in vacuo. 421 mg (1.30 mmol, 32%) (N-methyl-3-phenyl-N-(1-(thiazol-2-yl)piperidin-4-yl)propiolamide was obtained by CC (SiO2, 1.DCE 2.Chloroform). MS [MH+] 326.1

1. concentrationSubsequently, concentration
2. washwashed with water and brine
3. dry with materialdried over MgSO4
4. filtrationfiltered
5. concentrationconcentrated in vacuo