公开(公告)号：KR100303378B1

公开(公告)日：2001-09-24

申请号：KR1019990015261

申请日：1999-04-28

Applicant: 한국과학기술연구원

Inventor： 조용서 ,  최경일 ,  배애님 ,  고훈영 ,  김유승 ,  차주환 ,  이지은

IPC: C07D501/22

CPC classification number: Y02P20/55

Abstract: 일반식(V)로표시되는 3-히드록시세펨유도체와일반식(III)으로표시되는알릴할라이드또는일반식(IV)로표시되는아세틸렌할라이드를용매와금속촉매존재하에반응시켜신규일반식(I)로표시되는세팜유도체및 이의제조방법. 일반식(I)의화합물은세펨항생제제조에중요한중간체로사용할수 있다. 일반식(I)에있어서, R은페닐아세틸, 2-[2-아미노(1,3-티아졸-4-일)-2-(히드록시알콕시이미노)에틴닐, 2-[2-아미노(1,3-티아졸-4-일)-2-(알콕시이미노)에틴닐또는 4-히드록시페닐글라이신유도체를표시하며, R는수소, 카르복실산염(무기염으로나트륨및 칼륨염, 유기염으로알킬아민염, 방향족아민염)으로카르복시보호기로는 4-메톡시벤질, 디페닐메틸, 4-니트로벤질, 알릴등 세팔로스포린화합물분야에서의분자보호기를표시하며, Q로표시되는알킬화합물에서, R, R및 R는각각수소, 할로겐, 메틸, 에틸기의알킬기, 히드록시기, 페닐또는알콕시카보닐기를표시한다.

公开(公告)号：KR1020010029025A

公开(公告)日：2001-04-06

申请号：KR1019990041613

申请日：1999-09-28

Applicant: 한국과학기술연구원

Inventor： 고훈영 ,  조용서 ,  최경일 ,  배애님 ,  강경호 ,  이지은 ,  이희윤 ,  공재양 ,  정대영 ,  정선호

IPC: C07D413/06

Abstract: PURPOSE: Provided is a method for manufacturing an iso-oxazole piperazin compound and its salts which can end up developing a lead compound for new drugs. CONSTITUTION: An isooxazol compound is manufactured by the next step: reacting the compound of the formula (2) with the compound of the formula (3) at room temperature, at 0-7 deg.C, in the presence of organic solvent, 0.1-2 equivalent, preferably 1 equivalent of base, and chlorinating agent for 30 minutes-4 hours, preferably 2 hours. Wherein, organic solvent is selected from benzene, methylene chloride, and tetrahydrofuran; a base is selected from methyl amine, ethyl amine, diethyl amine, dimethyl amine, trimethyl amine, cyclohexylamine, diethylisopropylamine, pyridine, or preferably triethylamine; And chlorinating agent is one of chlorine, N-chlorosuccinimide, and sodium hypochlorite. In the formula (1), (2), and (3), R1 and R6 are a phenyl group, benzyl group, halide phenyl group, phenyl group having substituted C1-C6 alkyl group, phenyl group having substituted C1-C6 alkoxy group, methyl phenyl group, or pyridyl group. R2-R5 is hydrogen, and X is nitrogen.

Abstract translation: 目的：提供一种制造异恶唑哌嗪化合物及其盐的方法，其可以最终形成用于新药的铅化合物。 构成：通过下一步骤制备异恶唑化合物：在室温，0-7℃，有机溶剂存在下，将式（2）化合物与式（3）化合物反应，得到0.1 -2当量，优选1当量碱和氯化剂30分钟-4小时，优选2小时。 其中有机溶剂选自苯，二氯甲烷和四氢呋喃; 碱选自甲胺，乙胺，二乙胺，二甲胺，三甲胺，环己胺，二乙基异丙胺，吡啶，或优选三乙胺; 而氯化剂是氯，N-氯代琥珀酰亚胺和次氯酸钠之一。 在式（1），（2）和（3）中，R 1和R 6是苯基，苄基，卤化苯基，具有取代的C 1 -C 6烷基的苯基，具有取代的C 1 -C 6烷氧基的苯基 ，甲基苯基或吡啶基。 R2-R5是氢，X是氮。