NOVEL PROCESSES FOR THE PREPARATION OF 4-PHENYLPIPERIDINE DERIVATIVES

摘要

A process for preparing compound (E) from compound (A), with or without isolation of intermediate products, characterised by one or more of the following steps: (1) reacting the sulphonate compound (B) with the substituted phenol in the presence of a phase transfer catalyst and a base, (2) reacting compound (C) and the haloformate with addition of an HC1 scavenging base, (3) washing the reaction solution containing compound (D) with an aqueous acid selected from citric acid, phosphoric acid, acetic acid and formic acid, (4) heating compound (D) with sodium hydroxide to remove the carbamate group. Preferably the reaction(s) take place in toluene, providing an advantageous procedure for commercial production of paroxetine.