KITA JUNICHIRO,北 淳一郎,FUJIWARA HIROSHI,藤原 寛,TAKAMURA SHINJI,高村 真司
申请号：
JP2015137803
公开号：
JP2016006059A
申请日:
2015.07.09
申请国别(地区):
JP
年份:
2016
代理人:
摘要：
PROBLEM TO BE SOLVED: To provide a benzene sulfonic acid salt of (S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butanoic acid, that is excellent in anti-histaminic activity and anti-allergic activity, is low in acid addition salt hygroscopic property, and is excellent in physicochemical stability, and to provide a preparation thereof.SOLUTION: Provided is a benzene sulfonic acid salt of an optically active piperidine derivative, represented by formula (I), whose absolute configuration is in (S) form. Also provided is a synthesis method in which an optically active (S)-4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidine (IV) obtained by inducing an intermediate (±)-4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidine into a diastereomeric salt and optically resolving the same by fractional crystallization method, is used as the intermediate.COPYRIGHT: (C)2016,JPO&INPIT【課題】抗ヒスタミン活性及び抗アレルギー活性が優れ、酸付加塩の吸湿性が少なく、物理化学的安定性に優れる、(S)-4-〔4-〔(4-クロロフェニル)(2-ピリジル)メトキシ〕ピペリジノ〕ブタン酸のベンゼンスルホン酸塩及び該製法の提供。【解決手段】式(I)でで示される絶対配置が(S)体である光学活性ピペリジン誘導体のベンゼンスルホン酸塩。中間体である(±)-4-〔(4-クロロフェニル)(2-ピリジル)メトキシ〕ピペリジンをジアステレオマー塩に誘導し、これを分別結晶の方法で、光学分割して得られる光学活性な(S)-4-〔(4-クロロフェニル)(2-ピリジル)メトキシ〕ピペリジン(IV)を中間体として使用する合成方法。【選択図】なし
