公开(公告)号：KR1020030023968A

公开(公告)日：2003-03-26

申请号：KR1020010056740

申请日：2001-09-14

Applicant: 한국화학연구원

Inventor： 김봉진 ,  이철해 ,  김재학 ,  정희정 ,  편도규 ,  전미애 ,  권지웅 ,  김현주

IPC: C07D477/14

CPC classification number: Y02P20/55

Abstract: PURPOSE: Provided are carbapenem derivatives represented by formula(1) and a preparation method thereof. The carbapenem derivatives have antibacterial activity against the resistant strains such as methicillin resistant Staphylococcus aureus(MRSA) and resistant strain against Ofloxacin. CONSTITUTION: The method of preparation comprises: reacting a compound of formula(2) with a compound of formula(3) to make an ester derivatives of carbapenem represented by formula(4); and de-protecting carboxy group and hydroxy group. In formula(1), X is S or O atom; Y is hydrogen or halogen atom on a certain location in phenyl group, or C1-2 alkoxy group; M is hydrogen atom or a pair ion forming a pharmaceutically allowable salt. In formula(2,3 and 4), R1 is hydrogen atom or hydroxy protecting group; R2 is carboxy protecting group; X is S or O atom; Y is hydrogen or halogen atom on a certain location in phenyl group.

Abstract translation: 目的：提供式（1）表示的碳青霉烯衍生物及其制备方法。 碳青霉烯衍生物对抗性菌株如耐甲氧西林金黄色葡萄球菌（MRSA）和耐氧沙星的抗性菌株具有抗菌活性。 构成：制备方法包括：使式（2）化合物与式（3）化合物反应，制得由式（4）表示的碳青霉烯的酯衍生物; 并脱保护羧基和羟基。 在式（1）中，X是S或O原子; Y是苯基或C1-2烷氧基中某一位置上的氢或卤素原子; M是氢原子或形成药学上允许的盐的成对离子。 在式（2,3和4）中，R 1是氢原子或羟基保护基; R2是羧基保护基; X是S或O原子; Y是苯基中某一位置的氢或卤素原子。