Patent ID: 6610851
Filing Date: 2003-08-26
Classification: C07D

Abstract:
A method for preparing a piperidine compound represented by formula (VII): wherein R3 is a tert-butyl group,said method comprising the steps of: (A) reacting (3S,4R)-trans-4-(4-fluorophenyl)-3-hydroxymethylpiperidine represented by formula (II): with a protecting reagent represented by the formula (III): wherein R3 is as defined above, and Y is a tert-butoxycarbonyloxy group, in toluene, to give a carbamate compound represented by formula (IV): wherein R3 is as defined above; (B) reacting said carbamate compound with sulfonic acid chloride represented by formula (V): wherein R4 is an alkyl group having 1 to 2 carbon atoms or a phenyl group which may have a methyl group at the 4-position, to give a sulfonic acid ester represented by formula (VI): wherein R3 and R4 are as defined above, in the presence of triethylamine; and (C) mixing said sulfonic acid ester, toluene, 3,4-methylenedioxyphenol and sodium methylate methanol solution to react said sulfonic acid ester with 3,4-methylenedioxyphenol.