1-Methyl-4-piperidyl benzilate → 1-[2-(4-Benzyloxycarbonyl-phenyl)-ethyl]-4-(2-hydroxy-2,2-diphenyl-acetoxy)-1-methyl-piperidinium bromide

Participants

Reaction Conditions

Reaction Steps

Hydroxy-diphenyl-acetic-acid-1-methyl-piperidin-4-yl-ester (1.56 g, 4.8 mmol) and 4-(2-bromo-ethyl)-benzoic acid benzyl ester (2.3 ml, 7.21 mmol) are dissolved in DMF (5 ml) and stirred at 50° C. for 20 hours, followed by heating at 60° C. for 5 hours. Concentration and purification twice by C-18 reverse phase chromatography (eluant: water/acetonitrile) gives the title compound as a mixture of diastereoisomers.

Provenance & Evidence