Phosphorus oxide (P4O10) → 8-fluoro-7-trifluoromethyl-3,4-dihydro-2H-isoquinolin-1-one

Participants

Reaction Conditions

Reaction Steps

[2-(3-Fluoro-4-trifluoromethyl-phenyl)-ethyl]-carbamic acid ethyl ester (I-47c: 1.5 g, 5.376 mmol) was reacted with P2O5 (1.52 g, 10.75 mmol) and POCl3 (15 mL). The resulting mixture was refluxed for 1 hour at 110° C. to afford the crude product. Purification by column chromatography on silica gel (50% ethylacetate in hexane) afforded 350 mg of the product (27.97% yield).

Provenance & Evidence