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1. 发明公开

KR1020000065691A 항진균제용 터비나핀 및 그 염산염의 제조방법 有权
标题翻译：作为抗生素剂及其盐酸盐的生产酪氨酸蛋白酶
公开(公告)号：KR1020000065691A
公开(公告)日：2000-11-15
申请号：KR1019990012298
申请日：1999-04-08
申请人： 주식회사 씨트리 , 한솔케미언스 주식회사 , 고려제약주식회사
发明人： 이태석 , 안현숙 , 유창현 , 김경수 , 육진수 , 오성수 , 주소경 , 김완주
IPC分类号： C07C209/68
摘要： PURPOSE: A process for preparing the titled compound by using N-methyl-1-naphthalenemethaneamine or its hydrochloric acid salt and 1,3-dichloropropene as a starting material and reacting in the presence of a palladium catalyst system and an alkali is provided which produces a terbinafine compound in high yield and inhibits side reactions. CONSTITUTION: N-methyl-1-naphthalenemethaneamine or its hydrochloric acid salt and 1,3-dichloropropene are reacted with 0.5 to 5% by mole of a palladium catalyst selected from (PPh3)2PdCl2, (PhCN)2PdCl2 or (PPh3)4Pd in a nonpolar solvent in the presence of an alkali at 0 to 50°C for 1 to 2 hr to give N-methyl-N-(3-chloro-1-propene-2-yl)-naphthalenemethaneamine of formula (II), which is added with cul and amine, 3,3-dimethyl-1-butine successively to give (E)-terbinafine of formula (I).
摘要翻译：目的：提供使用N-甲基-1-萘甲烷或其盐酸盐和1,3-二氯丙烯作为原料并在钯催化剂体系和碱的存在下反应制备标题化合物的方法，其产生特比萘芬化合物高产量并抑制副反应。构成：将N-甲基-1-萘甲烷或其盐酸盐和1,3-二氯丙烯与0.5〜5摩尔％的选自（PPh 3）2 PdCl 2，（PhCN）2 PdCl 2或（PPh 3）4 Pd的钯催化剂反应，非碱性溶剂，在碱存在下，在0〜50℃下反应1〜2小时，得到式（II）的N-甲基-N-（3-氯-1-丙烯-2-基） - 萘甲烷胺，其中加入苦味胺和3,3-二甲基-1-丁胺，得到式（I）的（E） - 喋呤。

2. 发明授权

KR100293121B1 항진균제용 터비나핀 및 그 염산염의 제조방법 有权
标题翻译：特比萘芬及其盐酸盐作为抗真菌剂的制备方法
公开(公告)号：KR100293121B1
公开(公告)日：2001-06-15
申请号：KR1019990012298
申请日：1999-04-08
申请人： 주식회사 씨트리 , 한솔케미언스 주식회사 , 고려제약주식회사
发明人： 이태석 , 안현숙 , 유창현 , 김경수 , 육진수 , 오성수 , 주소경 , 김완주
IPC分类号： C07C209/68
摘要： 본발명은항진균제로서광범위한약효를갖는다음의구조식 (I)과 (Ia)로표시되는터비나핀및 그염산염의신규한제조방법을제공하기위한것이다. 본발명의방법은각 반응단계에서가장반응성이좋은촉매를선택함으로써하나의반응기에서약 2 내지 4시간의짧은시간내에반응을효율적으로수행하여터비나핀염산염을고순도, 고수율(약 70.5%)로합성하는것이다.

3. 发明授权

KR100286083B1 이미페넴의 제조방법 失效
标题翻译：制备IMIPENEM的方法
公开(公告)号：KR100286083B1
公开(公告)日：2001-03-15
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： 본발명은하기의반응식에따라, 일반식 (II)의비사이클릭케토에스테르를염기존재하에서포스포클로리데이트유도체와용매중에서축합시켜하기일반식 (III)의포스페이트유도체를제조하고; 같은반응용기내에서 2-아미노에탄티올의염산염을염기존재하에커플링시켜하기일반식 (IV)의티에나마이신유도체를제조하고; 같은반응용기내에서벤질이미데이트를가하여하기일반식 (V)의카르복실기가보호된이미페넴유도체를제조하고; 같은반응용기내에서테트라키스트리페닐포스핀팔라듐(0)과몰폴린유도체로보호기를제거하여하기일반식 (I)의이미페넴을제조하는방법에관한것이다. 상기식에서, X는수소또는클로라이드를나타낸다.

4. 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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