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1. 发明公开

KR1020000055522A 이미페넴의 제조방법 失效
标题翻译： IMIPENEM的合成方法
公开(公告)号：KR1020000055522A
公开(公告)日：2000-09-05
申请号：KR1019990004179
申请日：1999-02-08
申请人： 주식회사 씨트리
发明人： 김경수 , 이태석 , 육진수 , 윤정인 , 윤병훈 , 김완주
IPC分类号： C07D477/20
CPC分类号： Y02P20/55
摘要： PURPOSE: Provided is a synthetic method of imipenem which can easily remove a protecting group by using allyl group as the protecting group of 2-carboxy group. CONSTITUTION: A synthetic method comprises the steps of: condensing bicyclic ketoester of formula(II) and a phosphochloridate derivative in the presence of base to prepare a phosphate derivative of formula(III); coupling 2-aminoethantiol hydrochlorate with the produced phosphate derivative of formula(III) in the container to prepare a thienamycin derivative of formula(IV); reacting the produced thienamycin derivative of formula(IV) with benzylimidate in the container to prepare an imipenem derifative of formula(V) with carboxy group as a protecting group; and demasking the imipenem derivative produced using a moupholine dervative and tetrakis triphenylphosphin paladium.
摘要翻译：目的：提供亚胺培南的合成方法，通过使用烯丙基作为2-羧基的保护基，可以容易地除去保护基。构成：合成方法包括以下步骤：在碱存在下将式（II）的双环酮酯和磷酸氯代衍生物缩合制备式（III）的磷酸酯衍生物; 将所述产生的式（III）的磷酸酯衍生物与所述式（III）的磷酸酯衍生物偶联在容器中以制备式（IV）的噻吩霉素衍生物; 使制备的式（Ⅳ）噻吩甲酰胺衍生物与苄基亚氨酸酯在容器中反应以制备具有羧基作为保护基团的式（Ⅴ）亚胺培南衍生物; 并使用莫匹罗线虫和四苯基膦化合物制备亚胺培南衍生物。

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