Back to results
US 2003/0153753 A1Published application
Process for the preparation of a piperazine derivative
AssigneeAstellas Pharma Inc.
InventorsKeiichi Koga, Ryoki Orii, Yosuke Fujii, Shunsuke Goto, Satoshi Hirabayashi
Life of this patent
Estimating the term…
Abstract
(2R)-1-[3,5-bis(trifluoromethyl)benzoyl]-4-[2-[(2S)-2-(methoxymethyl)morpholino]ethyl]-2-(3-hydroxy-4-methylbenzyl)piperazine dihydrochloride is obtained by debenzylating (2R)-4-benzyl-1-[3,5-bis(trifluoromethyl)-benzoyl]-2-(3-hydroxy-4-methylbenzyl)piperazine, then N-alkylating and converting to hydrochloride.
Claims2
A process for preparing (2R)-1-[3,5-bis(trifluoro-methyl)benzoyl]-4-[2-[(2S)-2-(methoxymethyl)morpholino]-ethyl]-2-(3-hydroxy-4-methylbenzyl)piperazine dihydrochloride which is characterized by:
- (1) a step for debenzylating (2R)-4-benzyl-1-[3,5-bis(trifluoromethyl)benzoyl]-2-(3-hydroxy-4-methylbenzyl)-piperazine by reduction to produce (2R)-1-[3,5-bis(trifluoromethyl)benzoyl]-2-(3-hydroxy-4-methylbenzyl)-piperazine;
- (2) a step for subsequently 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) subsequent conversion of (2R)-1-[3,5-bis(trifluoromethyl)benzoyl]-4-[2-[(2S)-2-(methoxymethyl)-morpholino]ethyl]-2-(3-hydroxy-4-methylbenzyl)piperazine to hydrochloride.
Dependencies are inferred from the claim text.