Patent ID: 7501528
Filing Date: 2009-03-10
Classification: A61P,C07B,C07D

Abstract:
1. A method for preparing enantiomerically pure 4-pyrrolidino phenylbenzyl ether derivatives of the formula (I): said method comprising a) resolving a racemate of formula (II): with a resolving agent to obtain the (S)-enantiomer thereof of formula (S)-(II): b) converting the enantiomer of formula (S)-(II) into the corresponding primary amide of formula (III): and c) either directly reacting the compound of formula (III) with a compound of formula (IV): in the presence of at least acetic acid and/or acetic anhydride to obtain the compound of formula (I); or d) reacting the compound of formula (III) with a compound of formula (IV) to obtain a compound of formula (V): and then reacting the compound of formula (V) with an acetylating agent to obtain the compound of formula (I); wherein in the above formulae, Ar is an aryl group, optionally substituted by one or more substituent selected from the group consisting of halogen, nitro, cyano and (C R is (C R R n is 0, 1, 2 or 3.