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 DCM (10 ml). 2,2-Dimethyl-1,3-dioxolane-4-methanamine (216 mg; 1.65 mmol; 5 eq) and DIEA (0.17 ml; 0.98 mmol; 3 eq) are added. After one hour, the solvents are evaporated. The crude product is dissolved in DCM and washed with NH4Cl saturated solution, water and dried over MgSO4. After evaporation of the solvents, crude material is dissolved in DCM (3 ml). Title compound precipitates with addition diethyl ether, affording after filtration, Compound (14) as a white powder (65 mg; 46%).

1. customthe solvents are evaporated
2. dissolutionThe crude product is 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. dissolutionis dissolved in DCM (3 ml)
7. customTitle compound precipitates with addition diethyl ether
8. customaffording
9. filtrationafter filtration, Compound (14) as a white powder (65 mg; 46%)