1,1,1-Trifluoro-2,4-pentanedione → 1-(2-Amino-4-(trifluoromethyl)thiazol-5-yl)ethanone

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Reaction Steps

Hydroxy(tosyloxy)iodobenzene (3 g, 7.7 mmol) is added to a solution of 1,1,1,-trifluoro pentane-2,4-dione (1 g, 6.4 mmol) in ACN (10 mL). The resulting mixture is heated under reflux for 45 minutes, then cooled down to RT, and thiourea (0.59 g, 7.7 mmol) is added. The mixture is heated under reflux for 4 hours and then left to stand overnight. The reaction mixture is concentrated and the residue is recrystallised in ethylacetate and petroleum ether, affording 1-[2-amino-4-(trifluoromethyl)-1,3-thiazol-5-yl]ethanone (P8) as white solid (1.2 g, 79%).

Provenance & Evidence