Patent ID: 7229992

Claim:
A process for preparing (2R)-1-[3,5-bis(trifluoromethyl)benzoyl]-4-[2-[(2S)-2-(methoxymethyl)morpholino]ethyl]-2-(3-hydroxy-4-methylbenzyl)piperazine dihydrochloride, which comprises: (1) debenzylating (2R)-4-benzyl-1-[3,5-bis(trifluoromethyl)benzoyl]-2-(3-hydroxy-4-methylbenzyl)piperazine by chemical reduction with a hydride, a combination of metals or a metal compound with an organic acid or an inorganic acid to produce (2R)-1-[3,5-bis(trifluoromethyl)benzoyl]-2-(3-hydroxy-4-methylbenzyl)piperazine; (2) reacting (2R)-1-[3,5-bis(trifluoromethyl)benzoyl]-2-(3-hydroxy-4-methylbenzyl)piperazine with (2S)-4-(2-chloroethyl)-2-(methoxymethyl)morpholine or a salt thereof in the presence of a base to produce (2R)-1-[3,5-bis(trifluoromethyl)benzoyl]-4-[2-[(2S)-2-(methoxymethyl)morpholino]ethyl]-2-(3-hydroxy-4-methylbenzyl)piperazine; and (3) converting the (2R)-1-[3,5-bis(trifluoromethyl)benzoyl]-4-[2-[(2 S)-2-(methoxymethyl)morpholino]ethyl]-2-(3-hydroxy-4-methylbenzyl)piperazine to its hydrochloride salt.