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

関与物質

反応条件

反応手順

Trifluoroacetate salt of 4′-methyl-2-(morpholin-4-ylcarbonyl)-4,5′-bi-1,3-thiazol-2′-amine, prepared in Step II, described above (142.4 mg; 0.34 mmol; 1 eq.) is suspended in dry DCM (5 ml). CDI (108.8 mg; 0.68 mmol; 2 eq.) and triethylamine (511; 0.37 mmol; 1.10 eq.) are added. Some DMF (0.30 ml) is added to improve the solubility of the starting material. The mixture is stirred overnight at 40° C. A precipitate is formed. It is filtrated, washed with diethyl ether, affording N-[4′-methyl-2-(morpholin-4-ylcarbonyl)-4,5′-bi-1,3-thiazol-2′-yl]-1H-imidazole-1-carboxamide (107.1 mg; 79%) which is used as such in the next step without further purification.

情報源と証拠