Phosphorus oxychloride → HCID 86720177, compound

Participants

Reaction Conditions

Reaction Steps

To ethyl 2-hydroxy-4-methyl-7-(trifluoromethyl)-1,5-naphthyridine-3-carboxylate (1.05 g, 3.50 mmol, 1 eq.) was added POCl3 (11 ml) at RT and the reaction mixture was heated to reflux at 110° C. for 3 h. Afterwards excess POCl3 was distilled off and the residue was diluted with EtOAc (50 ml). The mixture was washed with a sat. solution of NaHCO3 (50 ml), water (50 ml), brine (50 ml), dried over anhydrous Na2SO4 and evaporated to provide ethyl 2-chloro-4-methyl-7-(trifluoromethyl)-1,5-naphthyridine-3-carboxylate (0.98 g, 3.08 mmol, 88%), which was used in subsequent reactions without further purification.

Provenance & Evidence