专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

US20100168433A1 PROCESS FOR PREPARING BEPOTASTINE AND INTERMEDIATES USED THEREIN 审中-公开
标题翻译：用于制备BEPOTASTINE及其中间体的方法
公开(公告)号：US20100168433A1
公开(公告)日：2010-07-01
申请号：US12663983
申请日：2008-06-05
申请人： Tae Hee Ha , Chang Hee Park , Won Jeoung Kim , Soohwa Cho , Han Kyong Kim , Kwee Hyun Suh
发明人： Tae Hee Ha , Chang Hee Park , Won Jeoung Kim , Soohwa Cho , Han Kyong Kim , Kwee Hyun Suh
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： A process for stereospecific preparation of bepotastine of formula (I) and novel intermediates used therein having formulae (II) to (IV) are provided. The inventive process comprises subjecting (RS)-4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidine to a reaction with a 4-halobutanoic acid l-menthyl ester, halo being chloro, bromo or iodo, in an organic solvent in the presence of a base to produce (RS)-bepotastine l-menthyl ester of formula (II), conducting a reaction of the compound of formula (II) with N-benzyloxycarbonyl L-aspartic acid in an organic solvent to induce selective precipitation of bepotastine l-menthyl ester.N-benzyloxycarbonyl L-aspartate of formula (III), filtering the precipitates formed in step 2) to isolate the compound of formula (III), treating the compound of formula (III) with a base to liberate bepotastine l-menthyl ester of formula (IV), and hydrolyzing the compound of formula (IV) in the presence of a base. The inventive process can provide bepotastine having a high optical purity of not less than 99.5% in a high yield, and thus, is useful in the development of anti-histamines and anti-allergic agents.
摘要翻译：提供了式（I）的贝他辛汀的立体特异性制备方法和其中使用的具有式（II）至（IV）的新型中间体。本发明的方法包括使（RS）-4 - [（4-氯苯基）（2-吡啶基）甲氧基]哌啶与4-卤代丁酸1-薄荷酯，卤素为氯，溴或碘的有机反应溶剂在碱的存在下反应以制备式（II）的（RS） - 贝斯塔司汀l-薄荷酯，在有机溶剂中进行式（II）化合物与N-苄氧基羰基L-天冬氨酸的反应，以诱导选择性贝他辛汀1-薄荷酯的沉淀。式（III）的N-苄氧基羰基L-天冬氨酸盐，过滤步骤2）中形成的沉淀物以分离式（III）化合物，用碱将式（III）化合物释放式（IV）的布他辛酯l-薄荷酯，并在碱的存在下水解式（IV）的化合物。本发明方法可以以高产率提供具有不低于99.5％的高光学纯度的贝他斯汀，因此可用于抗组胺和抗过敏剂的开发。

IPRDB

热门服务

关于我们

友情链接

联系方式