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1. 发明申请

WO2004097026B1 THE ENZYMATIC METHOD OF MAKING 1,2-DIOL DERIVATIVES AND THEIR ESTERS 审中-公开
标题翻译：制备1,2-二醇衍生物及其酯的方法
公开(公告)号：WO2004097026B1
公开(公告)日：2005-01-27
申请号：PCT/KR2004001005
申请日：2004-04-30
申请人： ENZYTECH LTD , HWANG SOON OOK , KIM DO HOON , RYU HYE YOUN
发明人： HWANG SOON OOK , KIM DO HOON , RYU HYE YOUN
IPC分类号： C12P7/02 , C12P7/62 , C12P41/00
CPC分类号： C12P7/02 , C12P7/62 , C12P41/004
摘要： The present invention relates to a new process for the preparation of optically active alcohols represented by the general formula 2 and their esters represented by the general formula 3 by enzymatic method from racemic alcohols represented by the general formula 1 in scheme 1. In more details, this invention relates to a process for producing optically active alcohols and their esters which are used as pharmaceutical intermediates from alcohols represented by the general formula 1 by stereospecific transesterification of secondary hydroxyl group using lipases as catalyst with acyl donors in organic solvent or with acyl donors only without using organic solvent. According to this invention, optically active alcohols and esters of high optical purity in high yield can be produced by transforming the primary hydroxyl group of 1,2-diols by tosyl group and transesterifying the secondary hydroxyl group stereospecifically by lipase.
摘要翻译：本发明涉及由方案1中由通式1表示的外消旋醇通过酶法由制备由通式2表示的光学活性醇及其由通式3表示的酯的新方法。更具体地，本发明涉及一种用于制备光学活性醇及其酯的方法，其通过使用脂肪酶作为催化剂的有机溶剂中的酰基供体的催化剂或仅与酰基供体的立体特异性酯交换作为由通式1表示的醇用作药物中间体不使用有机溶剂。根据本发明，可以通过将1,2-二醇的伯羟基转化为甲苯磺酰基并通过脂肪酶立体特异性酯交换酯酸化，可以制备高产率的高光学纯度的光学活性醇和酯。

2. 发明申请

WO2007108572A1 PROCESS FOR L-CARNITINE 审中-公开
标题翻译： L-CARNITINE的方法
公开(公告)号：WO2007108572A1
公开(公告)日：2007-09-27
申请号：PCT/KR2006/002003
申请日：2006-05-26
申请人： ENZYTECH, LTD. , HWANG, Soon Ook , CHUNG, Sun Ho
发明人： HWANG, Soon Ook , CHUNG, Sun Ho
IPC分类号： C07D303/40
CPC分类号： C07D303/40
摘要： The present invention relates to the process for the preparation of L-carnitine from racemic 3-acyloxy-gamma-butyrolactone or alkyl (R)-4-chloro-3-hydroxybutyrate. In more detail, this present invention relates to the process for the preparation of L-carnitine from (R)-3-hydroxy-gamma-butyrolactone, which was produced from racemic 3-acyloxy-gamma-butyrolactone by stereospecific hydrolysis using enzyme in the aqeous phase or organic phase including aqeous solvent or alkyl (R)-4-chloro-3-hydroxybutyrate, followed by a ring-opening reaction, epoxydation and a nucleophilic substitution by trimethylamine to prepare L-carnitine. The method of making L-carnitine is easier and more economical comparing to the con¬ ventional methods and L-carnitine produced has higher optical purity.
摘要翻译：本发明涉及由外消旋3-酰氧基-γ-丁内酯或（R）-4-氯-3-羟基丁酸烷基酯制备L-肉碱的方法。更详细地说，本发明涉及由（R）-3-羟基-γ-丁内酯制备L-肉碱的方法，该方法由外消旋3-酰氧基-γ-丁内酯通过立体特异性水解制得包括有机溶剂或（R）-4-氯-3-羟基丁酸烷基酯的有机相或有机相，随后进行开环反应，环氧化和用三甲胺进行亲核取代以制备L-肉碱。与常规方法相比，制备L-肉碱的方法更容易和更经济，并且生产的L-肉碱具有较高的光学纯度。

3. 发明申请

WO2005111227A1 THE METHOD OF MAKING OPTICALLY ACTIVE ESTER DERIVATIVES AND THEIR ACIDS FROM RACEMIC ESTERS 审中-公开
标题翻译：制备光学活性酯衍生物及其来自种子猕猴桃的方法
公开(公告)号：WO2005111227A1
公开(公告)日：2005-11-24
申请号：PCT/KR2005/001213
申请日：2005-04-27
申请人： EnzyTech, LTD. , HWANG, Soon Ook
发明人： HWANG, Soon Ook , CHUNG, Sun Ho
IPC分类号： C12P41/00
CPC分类号： C12P41/005 , C12P7/62 , C12P13/001 , C12P13/002
摘要： The present invention relates to process for the preparing of optically active ester derivatives and their acid derivatives which are used intensively as important chiral intermediates from racemic β-hydroxybutyl ester derivatives. In more detail, this invention relates to the process for preparing optically active β-hydroxybutyl ester derivatives and their acid derivatives by stere-ospecific hydrolysis of racemic β-hydroxybutyl ester derivatives using Upases or lipase-producing microorganisms in the aqeous phase or organic phase including aqeous solvent. The method of making optically active ester derivatives and their acid derivatives by hydrolysis of β-hydroxybutyl ester derivatives represented by the general formula 1 in scheme 1 is easier and more economical comparing to the conventional methods and the products have high optical purity. Also separation of ester derivatives from acid derivatives is easy after reaction. Thus this method is a useful process on the industrial scale.
摘要翻译：本发明涉及光学活性酯衍生物及其酸衍生物的制备方法，它们被广泛用作外消旋β-羟基丁酯衍生物的重要手性中间体。更详细地说，本发明涉及使用在酸性相或有机相中使用Upase或产生脂肪酶的微生物通过立体特异性水解外消旋β-羟基丁酯衍生物制备光学活性β-羟基丁酯衍生物及其酸衍生物的方法，包括有溶剂。通过水解方案1中通式1所示的β-羟基丁酯衍生物制备光学活性酯衍生物及其酸衍生物的方法比常规方法更容易和更经济，并且产品具有高的光学纯度。酯衍生物与酸衍生物的分离也很容易。因此，这种方法在工业规模上是一个有用的过程。

4. 发明申请

WO2004106534B1 THE ENZYMATIC METHOD OF MAKING 1,2-DIOL DERIVATIVES AND THEIR ESTERS WITH SUCCINE ANHYDRIDE 审中-公开
标题翻译：制备1,2-二醇衍生物的方法及其与无水异氰酸酯的酯化
公开(公告)号：WO2004106534B1
公开(公告)日：2005-06-16
申请号：PCT/KR2004001313
申请日：2004-06-02
申请人： ENZYTECH LTD , HWANG SOON OOK , KIM DO HOON , RYU HYE YOUN , LEE TAE IM , CHUNG SUN HO
发明人： HWANG SOON OOK , KIM DO HOON , RYU HYE YOUN , LEE TAE IM , CHUNG SUN HO
IPC分类号： C12P7/04 , C12P7/62 , C12P41/00
CPC分类号： C12P7/62 , C12P7/04 , C12P41/004
摘要： The present invention relates to a new process for the preparation of optically active alcohols represented by the general formula 2 and their esters represented by the general formula 3 in scheme 1. In more detail, this invention relates to the process for the preparation of optically active alcohols and their esters which are used as pharmaceutical intermediates by reacting the hydroxyl group stereospecifically by lipase after adding racemic alcohols represented by the general formula 1 and succinic anhydride as an acylating agent to the organic solvent. According to this invention, the primary hydroxyl group of 1,2-diols is transformed by other functional group and the secondary hydroxyl group is esterified stereospecifically with succinic anhydride as an acylating agent. Optically active alcohols and their esters of high optical purity in high yield can be produced by using succinic anhydride as an acylating agent because alcohols can be separated from their esters more easily than those of other conventional methods.
摘要翻译：本发明涉及制备由通式2表示的光学活性醇的新方法及其在方案1中由通式3表示的酯。更详细地说，本发明涉及制备光学活性的方法醇和它们的酯，其通过在将通式1表示的外消旋醇和琥珀酸酐作为酰化剂加入到有机溶剂中之后通过脂肪酶立体特异性地使羟基反应而用作药物中间体。根据本发明，1,2-二醇的伯羟基被其它官能团转变，仲羟基与琥珀酸酐作为酰化剂立体特异性酯化。通过使用琥珀酸酐作为酰化剂可以生产高产率的高光学纯度的光学活性醇及其酯，因为与其它常规方法相比，可以更容易地将醇与其酯分离。

5. 发明申请

WO2009151256A3 METHOD FOR PREPARING CLOPIDOGREL AND ITS DERIVATIVES 审中-公开
标题翻译：制备焦糖及其衍生物的方法
公开(公告)号：WO2009151256A3
公开(公告)日：2010-03-18
申请号：PCT/KR2009003083
申请日：2009-06-09
申请人： ENZYTECH LTD , HWANG SOON OOK , KIM KWANG SOO , KIM YOUNG JIN , JUNG CHEON OH
发明人： HWANG SOON OOK , KIM KWANG SOO , KIM YOUNG JIN , JUNG CHEON OH
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The present invention relates to a method for preparing Clopidogrel and its derivatives. More particularly, the present invention is a method for preparation of (S)-2-Clopidogrel and its derivatives, which are active inhibitors of platelet aggregation, from an optically active (S)-2-chlorophenylglycine alkyl ester through hydrolysis of racemic 2-chlorophenylglycine alkyl esters using an enzyme. The present invention employs a simple procedure to prepare Clopidogrel and its derivatives. Because no chiral resolving agents are used except for a small amount of enzyme, the cost of preparation can be reduced. In addition, the present invention is suitable for synthesizing highly optical-active Clopidogrel and its derivatives on a large scale by using optically active (S)-2-chlorophenylglycine alkyl ester obtained in high yield as an intermediate, and is also environmentally friendly since no highly toxic reagents are employed.
摘要翻译：本发明涉及氯吡格雷及其衍生物的制备方法。更具体地说，本发明是一种通过水解外消旋的2-氯苯基甘氨酸烷基酯从光学活性（S）-2-氯苯基甘氨酸烷基酯制备作为血小板聚集的活性抑制剂的（S）-2-氯吡格雷及其衍生物的方法，使用酶的氯苯基甘氨酸烷基酯。本发明采用简单的方法来制备氯吡格雷及其衍生物。由于除了少量的酶以外，不使用手性拆分剂，所以可以降低制备成本。另外，本发明适用于通过使用以高收率获得的光学活性（S）-2-氯苯基甘氨酸烷基酯作为中间体大规模合成高光活性氯吡格雷及其衍生物，并且也是环保的，因为没有使用高毒性试剂。

6. 发明申请

WO2007126258A1 THE METHOD OF MAKING OPTICALLY ACTIVE 2-HALO-2-(N-SUBSTITUTED PHENYL)ACETIC ACID ESTERS AND 2-HALO-2-(N-SUBSTITUTED PHENYL)ACETIC ACIDS BY ENZYMATIC METHOD 审中-公开
标题翻译：通过酶学方法制备光活性2-羟基-2-（N-取代的苯基）乙酸酯和2-羟基-2-（N-取代的苯基）乙酸的方法
公开(公告)号：WO2007126258A1
公开(公告)日：2007-11-08
申请号：PCT/KR2007/002073
申请日：2007-04-27
申请人： ENZYTECH, Ltd , HWANG, Soon Ook , CHUNG, Sun Ho
发明人： HWANG, Soon Ook , CHUNG, Sun Ho
IPC分类号： C07C51/09
CPC分类号： C12P7/54 , C12P41/005
摘要： The present invention relates to the process for the preparation of optically active 2-halo-2-(n-substituted phenyl)acetic acid esters and optically active 2-halo-2-(n-substituted phenyl)acetic acids, which are used intensively as important chiral intermediates, represented by general formula 2 and 3 respectively from racemic 2-halo-2-(n-substituted phenyl)acetic acid ester represented by general formula 1. In more detail, this invention relates to the process for preparing optically active 2-halo-2-(n-substituted phenyl)acetic acid esters and optically active 2-halo-2-(n-substituted phenyl)acetic acids by stereospecific hydrolysis of racemic 2-halo-2-(n-substituted phenyl)acetic acid esters using hydrolases or hydrolase-producing microorganisms in the aqueous phase or organic phase including aqueous solvent. This method is useful in the practical process because the production and separation of compounds with high optical purity is easier.
摘要翻译：本发明涉及光学活性2-卤代-2-（n-取代苯基）乙酸酯和光学活性2-卤代-2-（n-取代苯基）乙酸的制备方法，它们被广泛用于作为重要的手性中间体，分别由通式2和3分别由通式1表示的外消旋2-卤代-2-（正取代的苯基）乙酸酯代表。更详细地说，本发明涉及光学活性的制备方法 2-卤代-2-（正己基取代的苯基）乙酸酯和旋光性2-卤代-2-（n-取代的苯基）乙酸，通过外消旋的2-卤代-2-（n-取代的苯基）乙酸的立体特异性水解在水相或含有水溶剂的有机相中使用水解酶或水解酶产生微生物的酸酯。该方法在实际工艺中是有用的，因为具有高光学纯度的化合物的生产和分离更容易。

7. 发明申请

WO2007035066A1 THE METHOD OF MAKING OPTICALLY ACTIVE 3-ACYLOXY-GAMMA-BUTYROLACTONE AND OPTICALLY ACTIVE 3-HYDROXY-GAMMA-BUTYROLACTONE BY ENZYMATIC METHOD 审中-公开
标题翻译：通过酶学方法制备光学活性3-氰基 - 氨基 - 丁酸酯和光学活性3-羟基 - 马来酸 - 丁酯的方法
公开(公告)号：WO2007035066A1
公开(公告)日：2007-03-29
申请号：PCT/KR2006/003799
申请日：2006-09-25
申请人： ENZYTECH, LTD. , HWANG, Soon Ook , CHUNG, Sun Ho
发明人： HWANG, Soon Ook , CHUNG, Sun Ho
IPC分类号： C07D307/32
CPC分类号： C07D307/33
摘要： The present invention relates to the process for preparing optically active 3-acyloxy-gamma-butyrolactone repesented by the general formula 5 and optically active 3-hydroxy-gamma-butyrolactone represented by the general formula 6 in scheme 1 from racemic 3-acyloxy-gamma-butyrolactone repesented by the general formula 4 by enzymatic method. In more detail, this invention relates to the process for the preparation of optically active 3-acyloxy-gamma-butyrolactone and optically active 3-hydroxy-gamma-butyrolactone wherein racemic epichlorohydrin represented by the general formula 1 is subjected to produce racemic 4-chloro-3-hydroxybutyronitrile, racemic 3-hydroxy-gamma-butyrolactone and racemic 3-acyloxy-gamma-butyrolactone in turn and racemic 3-acyloxy-gamma-butyrolactone is hydrolyzed sterospecifically using lipases or lipase-producing microorganisms in the aqeous phase or organic phase containing water. This method is useful in the practical process because production and seperation of compounds with high optical purity are easy comparing with other reported process.
摘要翻译：本发明涉及由通式5制备的光学活性3-酰氧基-γ-丁内酯和方案1中由通式6表示的光学活性3-羟基-γ-丁内酯的方法，由外消旋3-酰氧基-γ 通过酶法测定通式4所代替的丁内酯。更详细地说，本发明涉及制备光学活性3-酰氧基-γ-丁内酯和光学活性3-羟基-γ-丁内酯的方法，其中由通式1表示的外消旋表氯醇经外消旋4-氯 -3-羟基丁腈，外消旋3-羟基-γ-丁内酯和外消旋3-酰氧基-γ-丁内酯依次和外消旋的3-酰氧基-γ-丁内酯在有机相或有机相中使用脂肪酶或产生脂肪酶的微生物进行空间特异性水解含水。该方法在实际工艺中是有用的，因为与其他报道的方法相比，具有高光学纯度的化合物的生产和分离容易。

8. 发明申请

WO2004106534A1 THE ENZYMATIC METHOD OF MAKING 1,2-DIOL DERIVATIVES AND THEIR ESTERS WITH SUCCINE ANHYDRIDE 审中-公开
标题翻译：制备1,2-二醇衍生物的方法及其与无水异氰酸酯的酯化
公开(公告)号：WO2004106534A1
公开(公告)日：2004-12-09
申请号：PCT/KR2004/001313
申请日：2004-06-02
申请人： ENZYTECH, LTD. , HWANG, Soon Ook , KIM, Do Hoon , RYU, Hye Youn , LEE, Tae Im , CHUNG, Sun Ho
发明人： HWANG, Soon Ook , KIM, Do Hoon , RYU, Hye Youn , LEE, Tae Im , CHUNG, Sun Ho
IPC分类号： C12P41/00
CPC分类号： C12P7/62 , C12P7/04 , C12P41/004
摘要： The present invention relates to a new process for the preparation of optically active alcohols represented by the general formula 2 and their esters represented by the general formula 3 in scheme 1. In more detail, this invention relates to the process for the preparation of optically active alcohols and their esters which are used as pharmaceutical intermediates by reacting the hydroxyl group stereospecifically by lipase after adding racemic alcohols represented by the general formula 1 and succinic anhydride as an acylating agent to the organic solvent. According to this invention, the primary hydroxyl group of 1,2-diols is transformed by other functional group and the secondary hydroxyl group is esterified stereospecifically with succinic anhydride as an acylating agent. Optically active alcohols and their esters of high optical purity in high yield can be produced by using succinic anhydride as an acylating agent because alcohols can be separated from their esters more easily than those of other conventional methods.
摘要翻译：本发明涉及制备由通式2表示的光学活性醇的新方法及其在方案1中由通式3表示的酯。更详细地说，本发明涉及制备光学活性的方法醇和它们的酯，其通过在将通式1表示的外消旋醇和琥珀酸酐作为酰化剂加入到有机溶剂中之后通过脂肪酶立体特异性地使羟基反应而用作药物中间体。根据本发明，1,2-二醇的伯羟基被其它官能团转变，仲羟基与琥珀酸酐作为酰化剂立体特异性酯化。通过使用琥珀酸酐作为酰化剂可以生产高产率的高光学纯度的光学活性醇及其酯，因为与其它常规方法相比，可以更容易地将醇与其酯分离。

9. 发明申请

WO2004097026A1 THE ENZYMATIC METHOD OF MAKING 1,2-DIOL DERIVATIVES AND THEIR ESTERS 审中-公开
标题翻译：制备1,2-二醇衍生物及其酯的方法
公开(公告)号：WO2004097026A1
公开(公告)日：2004-11-11
申请号：PCT/KR2004/001005
申请日：2004-04-30
申请人： ENZYTECH, LTD. , HWANG, Soon Ook , KIM, Do Hoon , RYU, Hye Youn
发明人： HWANG, Soon Ook , KIM, Do Hoon , RYU, Hye Youn
IPC分类号： C12P41/00
CPC分类号： C12P7/02 , C12P7/62 , C12P41/004
摘要： The present invention relates to a new process for the preparation of optically active alcohols represented by the general formula 2 and their esters represented by the general formula 3 by enzymatic method from racemic alcohols represented by the general formula 1 in scheme 1. In more details, this invention relates to a process for producing optically active alcohols and their esters which are used as pharmaceutical intermediates from alcohols represented by the general formula 1 by stereospecific transesterification of secondary hydroxyl group using lipases as catalyst with acyl donors in organic solvent or with acyl donors only without using organic solvent. According to this invention, optically active alcohols and esters of high optical purity in high yield can be produced by transforming the primary hydroxyl group of 1,2-diols by tosyl group and transesterifying the secondary hydroxyl group stereospecifically by lipase.
摘要翻译：本发明涉及由方案1中通式1表示的外消旋醇通过酶法由制备由通式2表示的光学活性醇及其由通式3表示的酯的新方法。更具体地，本发明涉及一种用于制备光学活性醇及其酯的方法，其通过使用脂肪酶作为催化剂的有机溶剂中的酰基供体的催化剂或仅与酰基供体的立体特异性酯交换作为由通式1表示的醇用作药物中间体不使用有机溶剂。根据本发明，可以通过将1,2-二醇的伯羟基转化成甲苯磺酰基并通过脂肪酶立体特异性酯交换酯化，可以制备高产率的高光学纯度的光学活性醇和酯。

10. 发明申请

WO2007139238A1 PROCESS FOR L-CARNITINE AND ACETYL L-CARNITINE HYDROCHLORIDE 审中-公开
标题翻译： L-卡尼丁和乙酰氯卡尼汀氢氯化物的方法
公开(公告)号：WO2007139238A1
公开(公告)日：2007-12-06
申请号：PCT/KR2006/002002
申请日：2006-05-26
申请人： ENZYTECH, LTD. , HWANG, Soon Ook , RYU, Hye Youn , CHUNG, Sun Ho
发明人： HWANG, Soon Ook , RYU, Hye Youn , CHUNG, Sun Ho
IPC分类号： C07C229/22
CPC分类号： C07C227/18 , C07C227/06 , C07C227/16 , C07C229/22
摘要： Provided is a process for preparing L-carnitine or acetyl L-carnitine hydrochloride. Specifically, the process comprises sequentially synthesizing racemic 4-chloro-3-hydroxybutyronitrile and racemic 4-chloro-3-hydroxy butyric acid alkyl ester under specific reaction conditions, using racemic epichlorohydrin as a starting material, preparing (R)-4-chloro-3-hydroxy butyric acid alkyl ester from stereoselective hydrolysis of the racemic 4-chloro-3-hydroxy butyric acid alkyl ester using an enzyme, and preparing L-carnitine or acetyl L-carnitine hydrochloride from the (R)-4-chloro-3-hydroxy butyric acid alkyl ester, according to the known method.
摘要翻译：提供了制备左旋肉碱或乙酰基左旋肉碱盐酸盐的方法。具体地说，该方法包括使用外消旋表氯醇作为起始原料，在特定的反应条件下依次合成外消旋的4-氯-3-羟基丁腈和外消旋的4-氯-3-羟基丁酸烷基酯，制备（R）使用酶从外消旋4-氯-3-羟基丁酸烷基酯的立体选择性水解制备3-羟基丁酸烷基酯，并从（R）-4-氯-3-三氟乙酸盐制备L-肉毒碱或乙酰基左旋肉碱盐酸盐 - 羟基丁酸烷基酯，按照已知方法。

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