Dimethylformamide → N-[4'-methyl-2-(morpholin-4-ylcarbonyl)-4,5'-bi-1,3-thiazol-2'-yl]-1H-imidazole-1-carboxamide

Participants

Reaction Conditions

Reaction Steps

In a 20 ml vial under Ar, triethylamine (51 μl; 0.37 mmol; 1.10 eq.) is added to a stirred suspension of 4′-methyl-2-(morpholin-4-ylcarbonyl)-4,5′-bi-1,3-thiazol-2′-amine, obtained in step II as describe above (142.4 mg; 0.34 mmol; 1 eq.), and CDI (54.4 mg; 0.34 mmol; 1 eq.) in dry DCM (5 ml). DMF (0.30 ml) is added to help the solubility. The mixture is stirred at 45° C. overnight. No starting material can be detected by HPLC. The reaction mixture is cooled down to RT. The resulting precipitate is isolated by filtration, washed with diethyl ether and dried under vacuum, affording Intermediate 7 (107.1 mg; 79%). It is used in the next step without further purification.

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