Phosphorus oxychloride → Methyl 4-chloro-8-fluoro-7-methylquinoline-2-carboxylate

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Reaction Steps

Methyl 8-fluoro-7-methyl-4-oxo-1,4-dihydroquinoline-2-carboxylate (7-7, 1.23 g, 5.23 mmol) in POCl3 (11 ml) was heated at 100° C. for 1 hour. The excess POCl3 was removed in vacuo. The resulting residue was triturated with ether, then filtered and washed with ether till no brown color remained in the ether. The remaining solid was Methyl 4-chloro-8-fluoro-7-methylquinoline-2-carboxylate (7-8, 993 mg, 75% yield) 100% pure by LCMS, LRMS m/z (M+H)+ 254.0 found, 254.1 required.

Provenance & Evidence