Triethylamine → N-[5-(5-{[[2-(Diethylamino)ethyl](methyl)amino]sulfonyl}-2-thienyl)-4-methyl-1,3-thiazol-2-YL]acetamide

Participants

Reaction Conditions

Reaction Steps

5-[2-(acetylamino)-4-methyl-1,3-thiazol-5-yl]thiophene-2-sulfonyl chloride, prepared as in Step II of Example 1 (500 mg; 1.48 mmol; 1.00 eq) is dissolved in DCM (30 ml). The solution is degassed with N2 and cooled down to 0° C. Triethylamine (1.0 ml; 7.42 mmol; 5.00 eq) followed by N,N-diethyl-N′-methylethylenediamine (1.2 ml; 7.42 mmol; 5.00 eq) are added. After 1 hour at 0° C., the reaction is complete. The reaction mixture is washed with NaHCO3 sat. (twice) and water (twice). The organic phase is dried over MgSO4, filtered and concentrated under vacuum, affording Compound (20) as a beige solid (570 mg; 89%).

Provenance & Evidence