Trimethyl orthoformate → 3-Fluoro-1-(2-fluoro-4-nitrophenyl)-4,4-dimethoxypiperidine

Participants

Reaction Conditions

Reaction Steps

The mixture of 4-(3-fluoro-4-oxo-piperidin-1-yl)-3-fluoronitrobenzene (65 mmol), trimethylorthoformate (130 mmol), p-toluene-sulphonic acid monohydrate (67 mmol) in methanol was heated at 45° C. for 24 hours. Solvent was removed and residual mass was taken into ethyl acetate and saturated sodium bicarbonate solution mixture. The organic layer was dried and removal of the solvent afforded title compound as a solid in 78% yield.

Provenance & Evidence