公开(公告)号：KR1020030021343A

公开(公告)日：2003-03-15

申请号：KR1020010054467

申请日：2001-09-05

Applicant: 한국과학기술연구원

Inventor： 조정혁 ,  오창현 ,  조한원

IPC: C07D487/02

Abstract: PURPOSE: Antibacterial carbapenem derivatives which are active against resistant strains are provided. They are pyrrolidine thiol carbapenems represented by formula(1), wherein R1 is hydrogen, substituted or unsubstituted lower alkly, heterocycles containing N or S, sulfonyl substituted with lower alkyl, carbonyl substituted with heterocycles containing N or S, benzyl, amide or hydroxy group; R2 is hydrogen, hydroxy alkyl, amide or ester group. CONSTITUTION: The method of preparation comprises: reacting phosphate compound with thiol derivatives represented by formula(2) under base and obtaining protected carbapenem derivatives; de-protecting them using hydrogen and palladium as a catalyst; and purifying with porous resin and freeze drying. In formula (2), R1 and R2 are same as in formula(1) and PNZ is p-nitrobenzyloxycarbonyl group.

Abstract translation: 目的：提供对抗性菌株有活性的抗菌碳青霉烯衍生物。 它们是由式（1）表示的吡咯烷硫醇碳青霉烯，其中R 1是氢，取代或未取代的低级烷基，含有N或S的杂环，被低级烷基取代的磺酰基，被含有N或S的杂环取代的羰基，苄基，酰胺或羟基 ; R2是氢，羟烷基，酰胺或酯基。 构成：制备方法包括：使磷酸酯化合物与式（2）表示的硫醇衍生物反应，并得到被保护的碳青霉烯衍生物; 使用氢和钯作为催化剂去保护它们; 并用多孔树脂进行纯化并冷冻干燥。 式（2）中，R 1和R 2与式（1）相同，PNZ为对硝基苄氧基羰基。

公开(公告)号：KR100441406B1

公开(公告)日：2004-07-23

申请号：KR1020010054467

申请日：2001-09-05

Applicant: 한국과학기술연구원

Inventor： 조정혁 ,  오창현 ,  조한원

IPC: C07D487/02

Abstract: PURPOSE: Antibacterial carbapenem derivatives which are active against resistant strains are provided. They are pyrrolidine thiol carbapenems represented by formula(1), wherein R1 is hydrogen, substituted or unsubstituted lower alkly, heterocycles containing N or S, sulfonyl substituted with lower alkyl, carbonyl substituted with heterocycles containing N or S, benzyl, amide or hydroxy group; R2 is hydrogen, hydroxy alkyl, amide or ester group. CONSTITUTION: The method of preparation comprises: reacting phosphate compound with thiol derivatives represented by formula(2) under base and obtaining protected carbapenem derivatives; de-protecting them using hydrogen and palladium as a catalyst; and purifying with porous resin and freeze drying. In formula (2), R1 and R2 are same as in formula(1) and PNZ is p-nitrobenzyloxycarbonyl group.

Abstract translation: 目的：提供对抗性菌株有活性的抗菌碳青霉烯衍生物。 它们是由式（1）表示的吡咯烷硫醇碳青霉烯类，其中R1是氢，取代或未取代的低级烷基，含有N或S的杂环，被低级烷基取代的磺酰基，被含有N或S的杂环取代的羰基，苄基，酰胺基或羟基 ; R2是氢，羟基烷基，酰胺或酯基。 构成：制备方法包括：使磷酸酯化合物与式（2）所示的硫醇衍生物在碱的作用下反应，得到被保护的碳青霉烯衍生物; 用氢和钯作为催化剂对其进行脱保护; 并用多孔树脂纯化并冷冻干燥。 式（2）中，R 1和R 2与式（1）相同，PNZ是对硝基苄氧基羰基。