Urea → Ethyl 2-amino-4-(trifluoromethyl)-1,3-oxazole-5-carboxylate

Participants

Reaction Conditions

Reaction Steps

To a suspension of urea (13.5 g) in DMF (50 mL) was added ethyl 4,4,4-trifluoro-2-chloroacetoacetate (10 mL) and the resulting reaction mixture was heated at 120° C. for 3 days. Then, the reaction mixture was cooled to RT and diluted with H2O (100 mL). Then, the reaction mixture was stirred at 0° C. for 1 h. The resulting precipitate was filtered, washed with H2O and dried in vacuo to yield ethyl 2-amino-4-trifluoromethyloxazole-5-carboxylate (A-1) as a white powder (9.8 g, 74% yield). LCMS (ESI) calcd for [M+1]+ 225.1. found 225.1.

Provenance & Evidence