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1. 发明授权

US06730809B2 Processes for the production of &agr;-difluoromethyl ornithine (DFMO) 有权
标题翻译：生产α-二氟甲基鸟氨酸（DFMO）的方法
公开(公告)号：US06730809B2
公开(公告)日：2004-05-04
申请号：US10224890
申请日：2002-08-19
申请人： Jingyang Zhu , Scott T. Chadwick , Benjamin A. Price , Shannon X. Zhao , Carrie A. Costello , Purushotham Vemishetti
发明人： Jingyang Zhu , Scott T. Chadwick , Benjamin A. Price , Shannon X. Zhao , Carrie A. Costello , Purushotham Vemishetti
IPC分类号： C07C25800
CPC分类号： C07C255/29 , C07C227/10 , C07C227/16 , C07C227/18 , C07C227/22 , C07C227/40 , C07C227/42 , C07C253/30 , C07C255/28 , C07C229/26
摘要： Provided are processes and synthetic intermediates useful for the preparation of &agr;-difluoromethylornithine (DFMO) having the formula
摘要翻译：提供了可用于制备具有下式的α-二氟甲基鸟氨酸（DFMO）的方法和合成中间体

2. 发明授权

US07012158B2 Processes for the production of α-difluoromethyl ornithine (DFMO) 有权
公开(公告)号：US07012158B2
公开(公告)日：2006-03-14
申请号：US10788728
申请日：2004-02-26
申请人： Jingyang Zhu , Scott T. Chadwick , Benjamin A. Price , Shannon X. Zhao , Carrie A. Costello , Purushotham Vemishetti
发明人： Jingyang Zhu , Scott T. Chadwick , Benjamin A. Price , Shannon X. Zhao , Carrie A. Costello , Purushotham Vemishetti
IPC分类号： C07C258/00 , C07C229/00
CPC分类号： C07C255/29 , C07C227/10 , C07C227/16 , C07C227/18 , C07C227/22 , C07C227/40 , C07C227/42 , C07C253/30 , C07C255/28 , C07C229/26
摘要： Provided are processes and synthetic intermediates useful for the preparation of α-difluoromethylornithine (DFMO) having the formula

3. 发明授权

US07141694B2 Enzymatic resolution of aryl and thio-substituted acids 失效
公开(公告)号：US07141694B2
公开(公告)日：2006-11-28
申请号：US10625403
申请日：2003-07-23
申请人： Jingyang Zhu , Shannon X. Zhao
发明人： Jingyang Zhu , Shannon X. Zhao
IPC分类号： C07C69/76 , C07C69/96
CPC分类号： H01M4/136 , C07C67/343 , C12P7/40 , C12P7/62 , C12P11/00 , C12P41/005 , H01M4/366 , H01M4/485 , H01M4/525 , H01M4/5825 , H01M4/625 , H01M10/052 , H01M10/0525 , H01M2004/027 , C07C69/738
摘要： Provided is a method of resolving a racemic mixture of a compound of formula I to obtain a desired enantiomer: wherein Ar is C6 or C10 aromatic group that can be substituted with H, C1 to C6 alkyl, trifluoromethyl or halo, R5 is halo or —S—R1, wherein R1 is H or acetyl, and R2 is H or C1 to C6 alkyl, the method comprising: reacting a compound of formula I wherein the compound is an ester whereby R2 is C1 to C6 alkyl with a lipase derived from Mucor meihei to stereoselectively hydrolyze the ester bond to produce an acid; and isolating the acid, wherein the reaction is conducted in a solvent comprising 80% to 98% v/v % organic phase and a residue of water phase (which can be buffered).

4. 发明授权

US06620600B2 Enzymatic resolution of aryl and thio-substituted acids 失效
标题翻译：芳基和硫取代的酸的酶解
公开(公告)号：US06620600B2
公开(公告)日：2003-09-16
申请号：US09946722
申请日：2001-09-05
申请人： Jingyang Zhu , Li You , Brenda J. White , Shannon X. Zhao , Paul M. Skonezny
发明人： Jingyang Zhu , Li You , Brenda J. White , Shannon X. Zhao , Paul M. Skonezny
IPC分类号： C12P1100
CPC分类号： H01M4/136 , C07C67/343 , C12P7/40 , C12P7/62 , C12P11/00 , C12P41/005 , H01M4/366 , H01M4/485 , H01M4/525 , H01M4/5825 , H01M4/625 , H01M10/052 , H01M10/0525 , H01M2004/027 , C07C69/738
摘要： Provided is a method of resolving a racemic mixture of a compound of formula I to obtain a desired enantiomer: wherein Ar is C6 or C10 aromatic group that can be substituted with H, C1 to C6 alkyl, trifluoromethyl or halo, R5 is halo or —S—R1, wherein R1 is H or acetyl, and R2 is H or C1 to C6 alkyl, the method comprising: reacting a compound of formula I wherein the compound is an ester whereby R2 is C1 to C6 alkyl with a lipase derived from Mucor meihei to stereoselectively hydrolyze the ester bond to produce an acid; and isolating the acid, wherein the reaction is conducted in a solvent comprising 80% to 98% v/v % organic phase and a residue of water phase (which can be buffered).
摘要翻译：提供一种拆分式I化合物的外消旋混合物以获得所需对映体的方法：其中Ar为可被H，C 1至C 6烷基，三氟甲基或卤素取代的C 6或C 10芳族基团，R 5为卤素或 - S-R1，其中R1是H或乙酰基，R2是H或C1-C6烷基，所述方法包括：使式I化合物，其中化合物是酯，其中R2是C1-C6烷基和衍生自毛霉素的脂肪酶咪唑立体选择性地水解酯键以产生酸; 并分离酸，其中反应在包含80％至98％v / v％有机相和水相残余物（可缓冲）的溶剂中进行。

5. 发明授权

US08558023B2 Enantioselective process for cycloalkenyl β-substituted alanines 有权
标题翻译：环烯基β-取代的丙氨酸的对映选择性方法
公开(公告)号：US08558023B2
公开(公告)日：2013-10-15
申请号：US13090632
申请日：2011-04-20
申请人： Zijun Liu , Sanhui Lin , Wenge Li , Jingyang Zhu , Xinjun Liu , Xiaojuan Zhang , Hui Lu , Fei Xiong , Zhongwei Tian
发明人： Zijun Liu , Sanhui Lin , Wenge Li , Jingyang Zhu , Xinjun Liu , Xiaojuan Zhang , Hui Lu , Fei Xiong , Zhongwei Tian
IPC分类号： C07C229/28 , C07C229/32
CPC分类号： C07C47/47 , C07C227/06 , C07C231/10 , C07C231/12 , C07C231/18 , C07C233/86 , C07C2601/10 , C07D209/52 , C07D263/42 , C07C229/28
摘要： A process for preparing an enantiomerically enriched cycloalkene-substituted alanine compound having the structure: by asymmetrically hydrogenating a dehydro amino acid compound having the structure: in a suitable reaction media in the presence of a catalyst having a transition metal moiety complexed to a chiral phosphine ligand to prepare enantiomerically enriched cycloalkene substituted alanine compounds having the structure of Formula (IA) or (IB), which are key intermediates for the ACE inhibitors ramipril and perindolpril:
摘要翻译：制备具有以下结构的对映体富集的环烯烃取代的丙氨酸化合物的方法：通过不对称地氢化具有以下结构的脱氢氨基酸化合物：在合适的反应介质中，在具有与手性膦配体复合的过渡金属部分的催化剂存在下，制备具有式（IA）或（IB）结构的对映体富集的环烯烃取代的丙氨酸化合物，其是ACE抑制剂雷米普利和perindolpril的关键中间体：

6. 发明授权

US07026143B2 Enzymatic resolution of aryl and thio-substituted acids 失效
标题翻译：芳基和硫取代的酸的酶解
公开(公告)号：US07026143B2
公开(公告)日：2006-04-11
申请号：US10625404
申请日：2003-07-23
申请人： Jingyang Zhu , Li You , Brenda J. White , Shannon X. Zha , Paul M. Skonezny
发明人： Jingyang Zhu , Li You , Brenda J. White , Shannon X. Zha , Paul M. Skonezny
IPC分类号： C12P11/00
CPC分类号： H01M4/136 , C07C67/343 , C12P7/40 , C12P7/62 , C12P11/00 , C12P41/005 , H01M4/366 , H01M4/485 , H01M4/525 , H01M4/5825 , H01M4/625 , H01M10/052 , H01M10/0525 , H01M2004/027 , C07C69/738
摘要： Provided is a method of resolving a racemic mixture of a compound of formula I to obtain a desired enantiomer: wherein Ar is C6 or C10 aromatic group that can be substituted with H, C1 to C6 alkyl, trifluoromethyl or halo, R5 is halo or —S—R1, wherein R1 is H or acetyl, and R2 is H or C1 to C6 alkyl, the method comprising: reacting a compound of formula I wherein the compound is an ester whereby R2 is C1 to C6 alkyl with a lipase derived from Mucor meihei to stereoselectively hydrolyze the ester bond to produce an acid; and isolating the acid, wherein the reaction is conducted in a solvent comprising 80% to 98% v/v % organic phase and a residue of water phase (which can be buffered).
摘要翻译：提供了一种拆分式I化合物的外消旋混合物以获得所需对映异构体的方法：其中Ar是可以被取代的C 6或C 10芳族基团 H，C 1至C 6烷基，三氟甲基或卤素，R 5是卤素或-SR 1，其中R 1是H或乙酰基，R 2是H或C 1 -C 6烷基，其中R 1是H或乙酰基，R 2是H或C 1 -C 6烷基，方法包括：使式I化合物，其中所述化合物是酯，其中R 2是C 1 -C 6烷基与脂肪酶衍生的从Mucor meihei到立体选择性地水解酯键以产生酸; 并分离酸，其中反应在包含80％至98％v / v％有机相和水相残余物（可缓冲）的溶剂中进行。

7. 发明申请

US20070167634A1 METHOD FOR PREPARING IRBESARTAN AND INTERMEDIATES THEREOF 有权
标题翻译：制备IRBESARTAN及其中间体的方法
公开(公告)号：US20070167634A1
公开(公告)日：2007-07-19
申请号：US11688635
申请日：2007-03-20
申请人： Edgar Miranda , Cornelis Vlaar , Jingyang Zhu
发明人： Edgar Miranda , Cornelis Vlaar , Jingyang Zhu
IPC分类号： C07D487/10
CPC分类号： C07D235/02 , C07D403/10
摘要： A method for preparing irbesartan and intermediates thereof. Irbesartan has the structure of formula I,
摘要翻译：厄贝沙坦及其中间体的制备方法。厄贝沙坦具有式I的结构，

8. 发明申请

US20100280245A1 PROCESS AND INTERMEDIATES FOR THE PREPARATION OF N-ACYLATED-4-ARYL BETA-AMINO ACID DERIVATIVES 有权
标题翻译：制备N-乙酰-4-氨基β-氨基酸衍生物的方法和中间体
公开(公告)号：US20100280245A1
公开(公告)日：2010-11-04
申请号：US12650128
申请日：2009-12-30
申请人： Shulin Wu , Bo Yu , Yejing Wang , Alain Delice , Jingyang Zhu
发明人： Shulin Wu , Bo Yu , Yejing Wang , Alain Delice , Jingyang Zhu
IPC分类号： C07D487/04 , C07C231/02 , C07C233/47
CPC分类号： C07D487/04 , C07B53/00 , C07B2200/07 , C07C269/06 , C07C271/22
摘要： A process for producing an enantiomerically enriched, pure or enriched and essentially pure compound of Formula I: wherein the R-, or S-configuration at the stereogenic center is marked with an *; which process hydrogenates an enamide compound of formula III: in an organic solvent in the presence of a transition metal precursor complexed to a chiral phosphine ligand catalyst; wherein Ar is phenyl which is unsubstituted or substituted; Z is OR1, SR1 and NR1R2; and P is R3, OR3, and NR3R4; R1 and R2 are selected from H, C1-8 alkyl, C5-12 cycloalkyl, aryl and aryl-C1-2-alkyl; or R1 and R2 together with the nitrogen atom to which they are attached form a C4-7-member heterocyclic ring system optionally fused with a 5- to 6-member carbocyclic or heterocyclic ring system; and R3 and R4 are selected from H, C1-8 alkyl, aryl, C5-12 cycloalkyl and aryl-C1-2-alkyl; or R3 and R4 together with the nitrogen atom to which they are attached form a C4-7-member heterocyclic ring system.
摘要翻译：制备对映异构体富集的，纯的或富集的和基本上纯的式I化合物的方法：其中立体中心处的R-或S-构型用*标记; 该方法使式III的酰胺化合物在有机溶剂中在与手性膦配位体催化剂络合的过渡金属前体存在下氢化; 其中Ar是未取代或取代的苯基; Z是OR1，SR1和NR1R2; 并且P是R 3，OR 3和NR 3 R 4; R 1和R 2选自H，C 1-8烷基，C 5-12环烷基，芳基和芳基-C 1-2 - 烷基; 或R 1和R 2与它们所连接的氮原子一起形成任选与5-至6-元碳环或杂环系统稠合的C 4-7元杂环系统; R 3和R 4选自H，C 1-8烷基，芳基，C 5-12环烷基和芳基-C 1-2 - 烷基; 或者R 3和R 4与它们所连接的氮原子一起形成C 4-7元杂环系。

9. 发明申请

US20100217013A1 ENANTIOSELECTIVE PROCESS FOR THE PREPARATION OF ZOLMITRIPTAN 审中-公开
标题翻译：用于制备ZOLMITRIPTAN的选择性方法
公开(公告)号：US20100217013A1
公开(公告)日：2010-08-26
申请号：US12638488
申请日：2009-12-15
申请人： Wenge Li , Yongxiang Chi , Jingyang Zhu
发明人： Wenge Li , Yongxiang Chi , Jingyang Zhu
IPC分类号： C07D209/14
CPC分类号： C07D209/14
摘要： An enantioselective process for preparing zolmitriptan, (S)-4-{[3-[2-(dimethylamine)ethyl]-1H-indol-5-yl]methyl}-2-oxazolidinone), by asymmetric hydrogenation of (Z)-2-(acetylamino)-3-{[3-N,N-(dimethylamine)ethyl)-1H-indol-5-yl]-2-propenoic acid methyl ester in the presence of hydrogen and an enantioselective chiral phosphine transition metal catalyst.
摘要翻译：（Z） - （S）-4 - {[3- [2-（二甲基胺）乙基] -1H-吲哚-5-基]甲基} -2-恶唑烷酮）的制备的对映选择性方法， 2-（乙酰氨基）-3 - {[3-N，N-（二甲基胺）乙基）-1H-吲哚-5-基] -2-丙烯酸甲酯在氢气和对映选择性手性膦过渡金属催化剂存在下。

10. 发明授权

US07388098B2 Dynamic resolution of isomers and resolved isomers 有权
标题翻译：动态拆分异构体和拆分的异构体
公开(公告)号：US07388098B2
公开(公告)日：2008-06-17
申请号：US09961932
申请日：2001-09-24
申请人： John J. Venit , Gary D. Madding , Victor W. Rosso , Francis J. Okuniewicz , Robert P. Discordia , Susanne Kiau , Atul S. Kotnis , Michael E. Randazzo , D. David Hennings , Jingyang Zhu , Jason G. Chen
发明人： John J. Venit , Gary D. Madding , Victor W. Rosso , Francis J. Okuniewicz , Robert P. Discordia , Susanne Kiau , Atul S. Kotnis , Michael E. Randazzo , D. David Hennings , Jingyang Zhu , Jason G. Chen
IPC分类号： C07C53/134 , C07D233/00 , C07D277/00 , C07B55/00
CPC分类号： C07D233/78 , C07C51/412 , C07C51/43 , C07C213/08 , C07C213/10 , C07D233/74 , C07C57/58
摘要： Provided is a dynamic resolution method of enriching a desired isomer of an alpha-substituted carboxylic acid relative to an undesired isomer, the method comprising: (a) in a solvent, contacting the alpha-substituted carboxylic acid, wherein the alpha substitution is with a leaving group and wherein the alpha carbon is chiral, with a homochiral amine to form a salt that is partially insoluble under selected reaction conditions, wherein the homochiral amine is selected so that the solubility of the amine salt of the undesired alpha-substituted carboxylic acid is greater than that of the amine salt of the desired alpha-substituted carboxylic acid under the selected reaction conditions; (b) reacting under the selected reaction conditions the salt with a nucleophile, wherein the reacting is effective in producing a net increase in the less soluble amine salt of the alpha-substituted carboxylic acid, and wherein the selected conditions are selected to (i) promote nucleophilic substitution of the nucleophile and the leaving group or (ii) to produce the increase in the less soluble amine salt in the absence of a strong base; and (c) maintaining the reaction for a period of time effective to increase the amount of the desired alpha-substituted carboxylic acid isomer.
摘要翻译：提供了相对于不期望的异构体富集α-取代的羧酸的所需异构体的动态拆分方法，该方法包括：（a）在溶剂中使α-取代的羧酸接触，其中α取代为离去基团，其中所述α碳是手性的，与同基因胺形成在所选择的反应条件下部分不溶的盐，其中选择所述同基因胺，使得不需要的α-取代羧酸的胺盐的溶解度为在选择的反应条件下大于所需α-取代羧酸的胺盐的浓度; （b）在所选择的反应条件下使所述盐与亲核试剂反应，其中所述反应有效地产生所述α-取代羧酸的较不溶性胺盐的净增加，并且其中所选择的条件选择为：（i）促进亲核试剂和离去基团的亲核取代，或（ii）在没有强碱的情况下产生较不溶性胺盐的增加; 和（c）保持反应一段时间有效以增加所需的α-取代的羧酸异构体的量。

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