Phosphorus oxychloride → 2-Chloro-4-methyl-7-(trifluoromethyl)quinoline-3-carboxylic acid ethyl ester

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Reaction Steps

A solution of 15.0 g (50.1 mmol) 2-hydroxy-4-methyl-7-(trifluoromethyl)quinoline-3-carboxylic acid ethyl ester in POCl3 (46 ml) was heated to 100° C. for 2 h. After cooling of the RS to RT, it was diluted with EtOAc and neutralised with a sat. aq. NaHCO3 sol. The organic phase was separated and washed with brine, dried over MgSO4 and concentrated in a vacuum. 15.4 g (48.5 mmol, 97%) 2-chloro-4-methyl-7-(trifluoromethyl)quinoline-3-carboxylic acid ethyl ester was obtained as a residue. The raw product was further converted without additional purification.

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