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1. 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。

2. 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。

3. 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。

4. 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。

5. 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。

6. 发明申请

WO2004020733A1 APPARATUS AND METHOD FOR AUTOMATICALLY DEFIBERING AND EXTRACTING KRAFT PULP FROM OLD CORRUGATED CARDBOARD 审中-公开
标题翻译：装置和方法，用于自动剔除和提取旧橡皮泥中的克拉夫浆
公开(公告)号：WO2004020733A1
公开(公告)日：2004-03-11
申请号：PCT/KR2002/001655
申请日：2002-09-02
申请人： GKP TECHNOLOGIES, INC. , CHUNG, Sun-Ho
发明人： CHUNG, Sun-Ho
IPC分类号： D21C5/02
CPC分类号： D21B1/345 , D21B1/32 , D21C5/02 , Y02W30/646 , Y02W30/648
摘要： The present invention relates to an apparatus and method for automatically defibering and extracting kraft pulp from old corrugated cardboards. The apparatus includes a) a pulper (1) for crushing, separating and defibering old corrugated cardboards using white water; b) a first means for continuously detecting defibering states of old corrugated cardboard pieces and outputting detected data; c) a second means for selectively exhausting defibered corrugated medium and linerboard from the pulper; d) a third means for respectively estimating first and second target values indicative of defibering states of corrugated medium and linerboard pieces defibered in the pulper (1); and a fourth means for controlling the second means to exhaust defibered corrugated medium and linerboard from the pulper (1) by comparing the detected data with the estimated first and second target values respectively. The first means has a comparative consistency meter (5) and the apparatus further includes a level meter (4) to detect the level of the white water in the pulper (1).
摘要翻译：本发明涉及一种用于从老瓦楞纸板自动切割和提取牛皮纸浆的设备和方法。该设备包括：a）使用白水破碎，分离和分解旧瓦楞纸板的碎浆机（1）; b）第一种连续检测旧瓦楞纸板切割状态并输出检测数据的装置; c）用于从碎浆机中选择性地排出脱纤维瓦楞纸介质和纸板的第二装置; d）第三装置，用于分别估计指示在碎浆机（1）中脱纤维的波纹状介质和衬板的脱纤维状态的第一和第二目标值; 以及第四装置，用于通过将检测到的数据与所估计的第一和第二目标值进行比较来控制第二装置以从碎浆机（1）排出脱纤维波纹介质和衬板。第一装置具有比较一致性计量器（5），并且该装置还包括用于检测碎浆机（1）中的白水水平的液位计（4）。

7. 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。

8. 发明申请

WO2007078176A1 THE METHOD OF MAKING OPTICALLY ACTIVE 2-CHLOROMANDELIC ACID ESTERS AND 2-CHLOROMANDELIC ACIDS BY ENZYMATIC METHOD 审中-公开
标题翻译：通过酶学方法制备光活性2-氯代酸酯和2-氯代苹果酸的方法
公开(公告)号：WO2007078176A1
公开(公告)日：2007-07-12
申请号：PCT/KR2007/000085
申请日：2007-01-05
申请人： ENZYTECH, LTD. , HWANG, Soon Ook , CHUNG, Sun Ho
发明人： HWANG, Soon Ook , CHUNG, Sun Ho
IPC分类号： C07C59/56
CPC分类号： C12P41/005 , C12P7/22 , C12P7/62
摘要： The present invention relates to process for the preparation of optically active 2-chloromandelic acid esters represented by the general formula 2 and optically active 2-chloromandelic acids represented by the general formula 2 which are used intensively as important chiral intermediates. In more detail, this invention relates to the process for preparing optically active 2-chloromandelic acid esters and optically active 2-chloromandelic acids by stereospecific hydrolysis of racemic 2-chloromandelic acid ester using lipases or lipase-producing microorganisms in the aqeous phase or organic phase including aqeous solvent. The method of making optically active 2-chloromandelic aicd esters and their acids is usful in the practical process because production of seperation of compounds with high optical purity are easy.
摘要翻译：本发明涉及制备由通式2表示的光学活性2-氯代扁桃酸酯和由通式2表示的光学活性2-氯代扁桃酸的方法，其被广泛用作重要的手性中间体。更详细地说，本发明涉及通过在酸性相或有机相中使用脂肪酶或产生脂肪酶微生物的外消旋2-氯扁桃酸酯的立体特异性水解制备光学活性2-氯扁桃酸酯和光学活性2-氯扁桃酸的方法包括有溶剂。制造光学活性的2-氯扁桃酸酯及其酸的方法在实际应用中是有用的，因为生产具有高光学纯度的化合物的分离是容易的。

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