反应详情

N-[5-(bromoacetyl)-4-methyl-1,3-thiazol-2-yl]acetamide, hydrobromide salt (Intermediate 1) (300 mg; 0.84 mmol; 1 eq) and 3-morpholin-4-yl-3-thioxo-propionamide (157.7 mg; 0.84 mmol; 1 eq) are dissolved in EtOH (10 ml). Triethylamine (0.29 ml; 2.09 mmol; 2.5 eq) is added. The mixture is stirred overnight at RT. Solvents are evaporated and the crude product is dissolved in EtOAc and washed with water, brine and dried over MgSO4. After filtration and evaporation of the solvents, the resulting yellow solid is dissolved in a DCM, Et2O and EtOH mixture. Concentration of this solution results in the precipitation of Compound (56) as yellow solid (126.2 mg; 41%)

1. customSolvents are evaporated
2. dissolutionthe crude product is dissolved in EtOAc
3. washwashed with water, brine
4. dry with materialdried over MgSO4
5. filtrationAfter filtration and evaporation of the solvents
6. dissolutionthe resulting yellow solid is dissolved in a DCM, Et2O and EtOH mixture