反应详情

Anhydrous magnesium sulfate (94 mg; 0.78 mmol; 4.15 eq.) and N-[5-(5-formyl-2-thienyl)-4-methyl-1,3-thiazol-2-yl]acetamide, Compound (1), (50 mg; 0.19 mmol; 1 eq.), are added to a solution of allylamine (17 μl ; 0.23 mmol; 1.20 eq.) and acetic acid (16 μl; 0.28 mmol; 1.50 eq.) in dry THF (5 ml). The reaction is stirred at rt overnight. The mixture is filtered and rinsed with anhydrous THF and DCM, affording N-(5-{5-[(E)-(allylimino)methyl]-2-thienyl}-4-methyl-1,3-thiazol-2-yl)acetamide which is used in the next step without further purification (57.3 mg, quantitative).

1. filtrationThe mixture is filtered
2. washrinsed with anhydrous THF and DCM