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1. 发明申请

WO2009084773A3 PREPARATION PROCESS USEFUL IN SYNTHESIS OF ATORVASTATIN 审中-公开
标题翻译：制备方法有利于合成ATORVASTATIN
公开(公告)号：WO2009084773A3
公开(公告)日：2010-02-18
申请号：PCT/KR2008001902
申请日：2008-04-04
申请人： CHO DONG-OCK , MEDICHEM KOREA CO LTD , KWON YOUNJA , CHA KYEONG-HOI , KIM YEONGSOOK , TAE HYUN-SEOP
发明人： CHO DONG-OCK , KWON YOUNJA , CHA KYEONG-HOI , KIM YEONGSOOK , TAE HYUN-SEOP
IPC分类号： C07D207/34 , C07D319/06 , C07D405/06
CPC分类号： C07D319/06 , C07D207/34 , C07D405/06
摘要： The present invention relates to a preparation process useful in synthesis of atorvastatin, more particularly a process for preparing atorvastatin is effective in treating hyperlipemia, comprising protecting the dihydroxy group at C3 and C5 positions of the starting material cis-t - butyl-6-substituted-3,5-dihydroxy-hexanoate with trialkyl orthoformate, reducing the terminal nitro or cyano group to amine group, performing JV-alkylation by sequentially reacting with ethyl 4-fluorobenzene-2-haloacetate and isobutyryl chloride, cyclizing with JV,3-diphenylpropynamide, and performing deprotection and hydrolysis.
摘要翻译：本发明涉及可用于合成阿托伐他汀的制备方法，更具体地说，一种制备阿托伐他汀的方法在治疗高脂血症方面是有效的，包括保护原料顺式叔丁基-6-取代的C3和C5位的二羟基 -3,5-二羟基己酸酯与原甲酸三烷基酯反应，将末端硝基或氰基还原成胺基，通过与4-氟苯-2-卤代乙酸乙酯和异丁酰氯依次反应进行N-烷基化，用JV，3-二苯基丙酰胺，进行脱保护和水解。

2. 发明申请

WO2003066619A1 METHOD FOR PURIFYING SIMVASTATIN 审中-公开
标题翻译：纯化SIMVASTATIN的方法
公开(公告)号：WO2003066619A1
公开(公告)日：2003-08-14
申请号：PCT/KR2003/000257
申请日：2003-02-06
申请人： CKD BIO CORPORATION , KIM, Jung Woo , KANG, Tae Won , PARK, Eui Seok , CHO, Dong Ock , BAEK, Hyeung Geun
发明人： KIM, Jung Woo , KANG, Tae Won , PARK, Eui Seok , CHO, Dong Ock , BAEK, Hyeung Geun
IPC分类号： C07D309/30
CPC分类号： C07D309/30
摘要： The present invention relates to a purification method of simvastatin crystal, more particularly to a method of effectively removing impurities contained in crude simvastatin obtained by a conventional synthetic method of simvastatin while minimizing loss of effective components to obtain high-quality simvastatin with good yield.
摘要翻译：本发明涉及辛伐他汀晶体的纯化方法，更具体地说，涉及一种有效去除通过常规的辛伐他汀合成方法获得的粗辛辛伐他汀所含杂质的方法，同时使有效成分的损失最小化，以获得高质量的辛伐他汀。

3. 发明申请

WO2006052066A1 PROCESS FOR PREPARING 1-ALPHA-HYDROXYCHOLECALCIFEROL DERIVATIVES 审中-公开
标题翻译：制备1-羟基羟基化合物衍生物的方法
公开(公告)号：WO2006052066A1
公开(公告)日：2006-05-18
申请号：PCT/KR2005/003681
申请日：2005-11-03
申请人： UK CHEMIPHARM CO., LTD. , OH, Gi-bum , KIM, Joon-seop , CHO, Dong-ock
发明人： OH, Gi-bum , KIM, Joon-seop , CHO, Dong-ock
IPC分类号： C07C401/00
CPC分类号： C07C401/00
摘要： Provided is a process for preparing a l-alpha-hydroxycholecalciferol derivative of Formula 7 with a high yield via a simplified reaction process, starting from a compound of Formula 1 having a structure similar to that of vitamin D3.
摘要翻译：提供了通过简化的反应过程从具有类似于维生素D3结构的式1化合物制备式7的1-α-羟基胆钙化甾醇衍生物以高产率制备的方法。

4. 发明申请

WO2009084773A2 PREPARATION PROCESS USEFUL IN SYNTHESIS OF ATORVASTATIN 审中-公开
标题翻译：制备方法用于合成ATORVASTATIN
公开(公告)号：WO2009084773A2
公开(公告)日：2009-07-09
申请号：PCT/KR2008/001902
申请日：2008-04-04
申请人： MEDICHEM KOREA. CO., LTD. , CHO, Dong-Ock , KWON, YounJa , CHA, Kyeong-Hoi , KIM, Yeongsook , TAE, Hyun-Seop
发明人： CHO, Dong-Ock , KWON, YounJa , CHA, Kyeong-Hoi , KIM, Yeongsook , TAE, Hyun-Seop
IPC分类号： C07D405/06 , C07D319/06
CPC分类号： C07D319/06 , C07D207/34 , C07D405/06
摘要： The present invention relates to a preparation process useful in synthesis of atorvastatin, more particularly a process for preparing atorvastatin is effective in treating hyperlipemia, comprising protecting the dihydroxy group at C3 and C5 positions of the starting material cis-t - butyl-6-substituted-3,5-dihydroxy-hexanoate with trialkyl orthoformate, reducing the terminal nitro or cyano group to amine group, performing JV-alkylation by sequentially reacting with ethyl 4-fluorobenzene-2-haloacetate and isobutyryl chloride, cyclizing with JV,3-diphenylpropynamide, and performing deprotection and hydrolysis.
摘要翻译：本发明涉及可用于合成阿托伐他汀的制备方法，更具体地说，一种制备阿托伐他汀的方法在治疗高脂血症方面是有效的，包括保护原料顺式叔丁基-6-取代的C3和C5位的二羟基 -3,5-二羟基己酸酯与原甲酸三烷基酯反应，将末端硝基或氰基还原成胺基，通过与4-氟苯-2-卤代乙酸乙酯和异丁酰氯依次反应进行N-烷基化，用JV，3-二苯基丙酰胺，进行脱保护和水解。

5. 发明申请

WO0145484A3 AN IMPROVED PROCESS FOR PREPARING SIMVASTATIN 审中-公开
标题翻译：制备SIMVASTATIN的改进方法
公开(公告)号：WO0145484A3
公开(公告)日：2002-03-28
申请号：PCT/KR0100301
申请日：2001-02-27
申请人： CHONG KUN DANG PHARM CORP , HONG CHUNG IL , KIM JUNG WOO , SHIN HEE JONG , KANG TAE WON , CHO DONG OCK
发明人： HONG CHUNG IL , KIM JUNG WOO , SHIN HEE JONG , KANG TAE WON , CHO DONG OCK
IPC分类号： A44C5/00 , A61K31/366 , A61P3/06 , A61P43/00 , C07B53/00 , C07D309/30
CPC分类号： C07D309/30 , Y02P20/55
摘要： The present invention relates to an improved process for preparing simvastatin and more particularly, the improved process for preparing simvastatin expressed by formula 1 with high yield and high purity by performing the following sequential processes comprising: (i) hydrolysis of lovastatin as starting material with potassium t-butoxide in an organic solvent and small amount of water under a mild reaction condition, followed by lactonization of the obtained solid intermediate with preventing from formation of by-products; (ii) protection of an alcohol group with t-butyldimethylsilyl group which can be easily removed with concentrated hydrochloric acid without the formation of by-products; (iii) acylation of the obtained protected intermediate with acyloxytriphenyl phosphonium salt as an acylating agent under a mild reaction condition; and (iv) removal of the silyl protective group with a concentrated hydrochloric acid. The present invention is to provide the improved process of preparing simvastatin expressed by formula 1 environmentally sound, economically efficient, and industrially useful.
摘要翻译：本发明涉及一种制备辛伐他汀的改进方法，更具体地说，涉及通过进行以下顺序方法制备具有高产率和高纯度的式1所表达的辛伐他汀的改进方法，包括：（i）将洛伐他汀作为原料与钾叔丁醇在有机溶剂和少量水中，在温和的反应条件下，然后将所得固体中间体内酯化，防止副产物的形成; （ii）用叔丁基二甲基甲硅烷基保护醇基，其可以用浓盐酸容易地除去而不形成副产物; （iii）在温和的反应条件下用酰氧基三苯基鏻盐作为酰化剂酰化所得保护的中间体; 和（iv）用浓盐酸除去甲硅烷基保护基。本发明提供了由式1表达的辛伐他汀的改进方法，其在环境无害，经济有效和工业上有用。

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