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公开(公告)号：KR100327758B1
公开(公告)日：2002-09-09
申请号：KR1019980036299
申请日：1998-09-03
IPC: C07D477/04 , C07D487/04
Abstract: PURPOSE: Carbapenem derivatives and a preparation process thereof are provided, thereby preparing carbapenem derivatives having improved antimicrobial activity and renal dehydropeptidase I(DHP-I) stability. CONSTITUTION: Carbapenem derivatives represented by formula(I) are provided, wherein R1 and R2 are independently hydrogen, hydroxy substituted or unsubstituted C1 to C5 lower alkyl, or allyl, and form C3 to C6 heterocycle containing nitrogen and optionally hetero atoms of S or O together; and X is carbonyl or sulfonyl. A process for preparing the carbapenem derivatives of formula(I) comprises the steps of: reacting carbapenem scaffold of formula(II) with diphenylchloro phosphate or anhydrous trifluoromethane sulfonic acid in the presence of base and a solvent to prepare a carbapenem intermediate of formula(VII); reacting the carbapenem intermediate of formula(VII) with thiol derivative of formula(III) in the presence of base and a solvent to prepare a protected carbapenem derivative of formula(VIII); and hydrogenating the protected carbapenem derivative of formula(VIII) in the presence of a catalyst to remove a protecting group, wherein R3 is para-nitrobenzyl or allyl; R4 is para-nitrobenzyloxycarbonyl or allyoxycarbonyl; X is carbonyl or sulfonyl; and Y is -OPO(OPh)2 or -OSO2CF3.
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公开(公告)号：KR1019990029501A
公开(公告)日：1999-04-26
申请号：KR1019980036299
申请日：1998-09-03
IPC: C07D477/04 , C07D487/04
Abstract: 본 발명은 일반식(I)로 표시되는 신규한 카바페넴 유도체 및 이들의 제조 방법에 관한 것이다. 이의 제조는 일반식(II)로 표시되는 카바페넴 모핵을 염기 존재하에 디페닐클로로포스페이트 또는 무수 트리플루오로메탄술폰산과 반응시켜 일반식(VII)로 표시되는 카바페넴 중간체를 제조하고, 이를 일반식(III)으로 표시되는 티올 유도체와 반응시켜 일반식(I)의 카바페넴 유도체를 제조하는 것으로, 이는 유용한 항생제로 사용할 수 있다.
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