Acetonitrile → Methyl 4-({1-[2-(4-cyanophenyl)ethyl]-4-hydroxypiperidin-4-ylmethyl}amino)benzoate

Participants

Reaction Steps

A mixture of the compound (242 mg) obtained in Step 3 of Example 1, methyl 4-aminobenzoate (756 mg), anhydrous lithium perchlorate (106 mg) and anhydrous acetonitrile (1 mL) was heated under reflux for two hours under nitrogen atmosphere. To the mixture was added brine (5 mL) and the residue was extracted with ethyl acetate. The organic layer was washed with brine and dried over anhydrous sodium sulfate. The solid residue obtained by removal of the solvent was washed two times by suspending in tert-butyl methyl ether to obtain the titled compound (144 mg) as powder.

Provenance & Evidence