反应详情

5-[2-(acetylamino)-4-methyl-1,3-thiazol-5-yl]thiophene-2-sulfonyl chloride, prepared as in Step II of Example 1 (110 mg; 0.33 mmol; 1 eq), is dissolved in DMF (10 ml). Dimethylamine (0.1 ml; 1.65 mmol; 5 eq) and DIEA (0.17 ml; 0.98 mmol; 3 eq) are added. After one hour, the solvents are evaporated to dryness. The crude product is re-dissolved in DCM and washed with NH4Cl saturated solution, water and dried over MgSO4. After evaporation of the solvents, crude material is precipitated in a mixture of DCM and diethyl ether, affording after filtration, Compound (18) as a yellow powder (52 mg; 46%).

1. customthe solvents are evaporated to dryness
2. dissolutionThe crude product is re-dissolved in DCM
3. washwashed with NH4Cl saturated solution, water
4. dry with materialdried over MgSO4
5. customAfter evaporation of the solvents, crude material
6. customis precipitated in a mixture of DCM and diethyl ether
7. customaffording
8. filtrationafter filtration, Compound (18) as a yellow powder (52 mg; 46%)