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1. 发明授权

US12104022B2 Chiral resolution method mimicking magnetic beneficiation and the magnetic nano-inhibitors for selective enrichment 有权
公开(公告)号：US12104022B2
公开(公告)日：2024-10-01
申请号：US17267156
申请日：2019-04-09
申请人： PEKING UNIVERSITY
发明人： Xinhua Wan , Xichong Ye , Bowen Li , Jie Zhang
IPC分类号： C08J3/215 , B03C1/005 , B03C1/01 , B03C1/015 , B03C1/02 , B03C1/035 , B03C1/28 , B82Y30/00 , C07B57/00 , C07C227/34 , C07C231/20 , C07C231/24 , C08F212/08 , C08F220/56 , C08F220/58 , C08F293/00 , C08J3/24 , C08K3/22 , C08K5/09 , C08K9/10 , B82Y25/00 , B82Y40/00 , C07C237/06 , C08F220/60
CPC分类号： C08J3/215 , B03C1/005 , B03C1/01 , B03C1/015 , B03C1/02 , B03C1/035 , B03C1/286 , C07B57/00 , C07C227/34 , C07C231/20 , C07C231/24 , C08F212/08 , C08F220/56 , C08F220/58 , C08F293/005 , C08J3/245 , C08K3/22 , C08K5/09 , C08K9/10 , B03C2201/18 , B03C2201/26 , B82Y25/00 , B82Y30/00 , B82Y40/00 , C07B2200/07 , C07C237/06 , C08F220/603 , C08F2438/03 , C08J2325/08 , C08K2003/2275 , C08K2201/003 , C08K2201/01 , C08K2201/011 , C07C227/34 , C07C229/36 , C07C227/34 , C07C229/22 , C07C231/20 , C07C237/06
摘要： A core-shell nanocomposite is formed by co-assembly of an amphiphilic polymer and hydrophobically modified magnetic nanoparticles, with its core being a hydrophobically modified magnetic nanomaterial and its shell being the amphiphilic polymer, wherein hydrophilic segments in the amphiphilic polymer are located at an outermost layer of the shell. The above composite can be used as additives in the crystallization of conglomerates and obtain optically pure crystals of both enantiomers in a single process. The key thereof is that the composite is used to enrich molecules with the same configuration while inhibit the crystallization of the other enantiomer in a supersaturated solution of conglomerates, such that a non-magnetic crystal and a magnetic crystal (which are enantiomers of each other) are generated in a unit operation. Optically pure crystals of both enantiomers with over 90 ee % can be obtained by one-time crystallization, and the total yield can be as high as 40%.

2. 发明申请

US20130178651A1 PREPARATION METHOD OF HIGH-OPTICAL PURITY N2-[1-(S)-ETHOXYCARBONYL-3-PHENYLPROPYL]-N6-TRIFLUOROACETYL-L-LYSINE 有权
标题翻译：高光固化N2- [1-（S） - 乙氧羰基-3-苯基丙基] -N6-三氟乙酰基-L-赖氨酸的制备方法
公开(公告)号：US20130178651A1
公开(公告)日：2013-07-11
申请号：US13822690
申请日：2010-09-29
申请人： Limin Que , Yueheng Jiang , Zhigang Lin , Tong Cai
发明人： Limin Que , Yueheng Jiang , Zhigang Lin , Tong Cai
IPC分类号： C07C51/42
CPC分类号： C07C51/42 , C07B2200/07 , C07C231/20 , C07C233/47
摘要： Disclosed is a preparation method of high-optical purity N2-[1-(S)-ethoxycarbonyl-3-phenylpropyl]-N6-trifluoroacetyl-L-lysine. The method includes: adding crude N2-[1-(S)-ethoxycarbonyl-3-phenylpropyl]-N6-trifluoroacetyl-L-lysine to one or more organic solvents, and then reacting with an organic acid to form a salt, which is precipitated, thereby achieving the purpose of separation and purification; next, adding the obtained solid or mother concentrate into deionized water, and then adding an inorganic base or an organic base for basification, so as to adjust the pH value, removing the organic acid, filtering, washing and drying, to obtain the high-optical purity N2-[1-(S)-ethoxycarbonyl-3-phenylpropyl]-N6-trifluoroacetyl-L-lysine, where the molar ratio of 1S-isomer to 1R-isomer is equal to or greater than 99:1.
摘要翻译：公开了高光学纯度N2- [1-（S） - 乙氧基羰基-3-苯基丙基] -N6-三氟乙酰基-L-赖氨酸的制备方法。该方法包括：向一种或多种有机溶剂中加入粗N2- [1-（S） - 乙氧基羰基-3-苯基丙基] -N6-三氟乙酰基-L-赖氨酸，然后与有机酸反应形成盐，沉淀，从而达到分离纯化的目的; 然后，将得到的固体或母体浓缩物加入去离子水中，然后加入无机碱或有机碱进行碱化，调节pH值，除去有机酸，过滤，洗涤和干燥，光学纯度N2- [1-（S） - 乙氧基羰基-3-苯基丙基] -N6-三氟乙酰基-L-赖氨酸，其中1S-异构体与1R-异构体的摩尔比等于或大于99:1。

3. 发明申请

US20130131359A1 PROCESSES AND INTERMEDIATES FOR PREPARING STERIC COMPOUNDS 审中-公开
标题翻译：制备化合物的方法和中间体
公开(公告)号：US20130131359A1
公开(公告)日：2013-05-23
申请号：US13740707
申请日：2013-01-14
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： GERALD J. TANOURY , Minzhang Chen , Young Chun Jung , Raymond E. Forslund
IPC分类号： C07C231/12 , C07C247/06 , C07C59/255 , C07J75/00 , C07J9/00 , C07D303/48 , C07C51/41
CPC分类号： C07C231/12 , C07B2200/05 , C07B2200/07 , C07C51/412 , C07C59/255 , C07C231/20 , C07C237/04 , C07C247/04 , C07C247/06 , C07C2601/02 , C07D209/52 , C07D301/14 , C07D303/48 , C07D401/14 , C07D403/12 , C07D403/14 , C07D498/10 , C07J9/005 , C07J75/00 , C07K5/0202 , C07K7/02
摘要： This invention relates to processes and intermediates for the preparation of an alpha-amino beta-hydroxy acid of Formula 1 wherein the variables R1, R′1 and R2 are defined herein and the compound of Formula 1 has an enantiomeric excess (ee) of 55% or greater.
摘要翻译：本发明涉及用于制备式1的α-氨基β-羟基酸的方法和中间体，其中变量R1，R'1和R2在本文中定义，式1的化合物具有55的对映体过量（ee）％以上。

4. 发明授权

US08222454B2 Process for preparing optical pure milnacipran and its pharmaceutically accepted salts 失效
标题翻译：制备光学纯米那普仑及其药学上可接受的盐的方法
公开(公告)号：US08222454B2
公开(公告)日：2012-07-17
申请号：US12517379
申请日：2007-11-28
申请人： Lin Ai , Xiao Liu
发明人： Lin Ai , Xiao Liu
IPC分类号： C07C233/58
CPC分类号： C07C231/20 , C07B2200/07 , C07C2601/02 , C07C237/24
摘要： The present invention discloses a process for preparing optically pure milnacipran and their pharmaceutically acceptable salts, which adopts racemic milnacipran as starting material, tartaric acid derivatives and their compositions as resolving agents to resolve.
摘要翻译：本发明公开了一种制备光学纯米那普仑及其药学上可接受的盐的方法，其采用外消旋米那普兰作为起始原料，酒石酸衍生物及其组合物作为分离剂进行分解。

5. 发明申请

US20120016151A1 PROCESS FOR MANUFACTURE AND RESOLUTION OF 2-ACYLAMINO-3-DIPHENYLPROPANOIC ACID 有权
标题翻译： 2-氨基亚氨基-3-二苯基丙酸的制备和分解方法
公开(公告)号：US20120016151A1
公开(公告)日：2012-01-19
申请号：US13144340
申请日：2010-01-12
申请人： Guoliang Zhu , Lijun Yang , Ying Lin , Jie Ying
发明人： Guoliang Zhu , Lijun Yang , Ying Lin , Jie Ying
IPC分类号： C07C229/36
CPC分类号： C07C231/12 , C07B53/00 , C07B2200/07 , C07C231/20 , C07C233/47 , C07C233/87
摘要： The invention relates to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors.
摘要翻译：本发明涉及可用于合成药物活性化合物，特别是中性肽链内切酶（NEP）抑制剂的新方法，新方法步骤和新型中间体。

6. 发明申请

US20090187017A1 PROCESS FOR PREPARING ENANTIOMERICALLY ENRICHED BETA-AMINO ACID DERIVATIVES 审中-公开
标题翻译：制备高效β-氨基酸衍生物的方法
公开(公告)号：US20090187017A1
公开(公告)日：2009-07-23
申请号：US12064194
申请日：2006-07-25
申请人： Albrecht Berkessel , Felix Cleemann , Santanu Mukherjee
发明人： Albrecht Berkessel , Felix Cleemann , Santanu Mukherjee
IPC分类号： C07D265/06 , C07C233/87
CPC分类号： C07B57/00 , C07B2200/07 , C07C231/20 , C07D265/06 , C07C233/87
摘要： The present invention relates to a process for the organo-catalysed kinetic racemate resolution of compounds of the general formula (II). It is thus possible through the action of catalytic amounts of enantiomerically enriched compounds of the general formula (Ia) or (Ib) to obtain on the one hand enantiomerically enriched optionally N-acylated β-amino acid esters and on the other hand enantiomerically enriched 4,5-dihydrooxazin-6-ones (oxazinones). The corresponding enantiomerically enriched β-amino acids can be formed from both easily separable classes of compounds by simple hydrolysis.
摘要翻译：本发明涉及通式（Ⅱ）化合物的有机催化动力学外消旋体拆分方法。因此，通过催化量的通式（Ia）或（Ib）的对映异构体富集的化合物的作用可以一方面获得对映体富集的任选N-酰化的β-氨基酸酯，另一方面获得对映体富集的4 ，5-二氢恶嗪-6-酮（恶嗪酮）。相应的对映异构体富集的β-氨基酸可以通过简单水解由容易分离的化合物类型形成。

7. 发明授权

US07199264B2 Method of resolving optical isomers of amino acid derivative 失效
标题翻译：拆分氨基酸衍生物的光学异构体的方法
公开(公告)号：US07199264B2
公开(公告)日：2007-04-03
申请号：US10415559
申请日：2001-10-25
申请人： Shin Watanabe , Mizue Kawahara
发明人： Shin Watanabe , Mizue Kawahara
IPC分类号： C07B55/00
CPC分类号： C07C269/08 , C07B2200/07 , C07C231/20 , C07C319/28 , C07D207/16 , C07C233/83 , C07C271/22 , C07C323/58 , C07C323/59
摘要： Provided is a separating method for an optical isomer mixture comprising the steps of mixing an amino acid derivative such as N-(tert-butoxycarbonyl)-DL-alanine in which optical isomers of a D type and an L type are present in a mixture with a hydrophilic compound such as β-cyclodextrin having a different affinity to two kinds of the optical isomers described above and then bringing the resulting aqueous solution or aqueous suspension into contact with a hydrophobic substance such as a solid matter subjected on a surface thereof to hydrophobic treatment on the condition that the pH is 3.5 or lower or under the coexistence of ions including an atomic group having hydrophobicity which can be a counter ion for the amino acid derivative described above such as a triethylammonium ion to thereby separate the D type amino acid derivative from the L type amino acid derivative present in the above aqueous solution or aqueous suspension.
摘要翻译：本发明提供了一种旋光异构体混合物的分离方法，包括将混合物中存在D型和L型光学异构体的氨基酸衍生物如N-（叔丁氧羰基）-DL-丙氨酸混合物混合物对上述两种旋光异构体具有不同亲和性的亲水性化合物如β-环糊精，然后将所得水溶液或水悬浮液与其表面经受的固体物质等疏水性物质接触，进行疏水处理在pH为3.5以下或者含有具有疏水性的原子团的离子共存的情况下，其可以是上述氨基酸衍生物的反离子，例如三乙基铵离子，从而将D型氨基酸衍生物从存在于上述水溶液或水性悬浮液中的L型氨基酸衍生物。

8. 发明授权

US06271263B1 Compositions containing and methods of using 1-aminoindan and derivatives thereof and process for preparing optically active 1-aminoindan derivatives 有权
标题翻译：包含使用1-氨基茚丹及其衍生物的组合物和制备光学活性1-氨基茚满衍生物的方法
公开(公告)号：US06271263B1
公开(公告)日：2001-08-07
申请号：US09260755
申请日：1999-03-02
申请人： Benjamin Sklarz , Ramy Lidor , Eliezer Bahar , Yaacov Herzig , Jeff Sterling , Alex Veinberg
发明人： Benjamin Sklarz , Ramy Lidor , Eliezer Bahar , Yaacov Herzig , Jeff Sterling , Alex Veinberg
IPC分类号： A01N3718
CPC分类号： C07C237/04 , A61K31/135 , A61K31/136 , A61K31/137 , A61K31/165 , A61K31/166 , A61K31/167 , A61K31/18 , A61K31/195 , A61K31/196 , A61K31/215 , A61K31/216 , A61K31/24 , A61K31/27 , A61K31/275 , A61K31/277 , C07C209/04 , C07C209/88 , C07C211/38 , C07C211/42 , C07C213/10 , C07C215/44 , C07C217/52 , C07C217/74 , C07C231/20 , C07C233/03 , C07C233/06 , C07C233/11 , C07C233/14 , C07C233/23 , C07C233/52 , C07C233/65 , C07C233/74 , C07C235/54 , C07C237/22 , C07C237/48 , C07C255/24 , C07C255/58 , C07C271/22 , C07C2602/08 , C07C2602/10 , A61K31/19 , A61K2300/00
摘要： Novel derivatives of 1-aminoindan and their salts are described. Optically active 1-aminoindan derivatives are prepared by reacting a N-benzyl analog of the desired compound with an enantiomer of mandelic acid. Parkinson's disease, dementia, epilepsy, convulsions, or seizures are treated by administering a compound of the formula:
摘要翻译：描述了1-氨基茚满及其盐的新型衍生物。通过使所需化合物的N-苄基类似物与扁桃酸的对映异构体反应来制备光学活性的1-氨基茚满衍生物。帕金森病，痴呆，癫痫，抽搐或癫痫发作通过给予下列化学式来治疗：

9. 发明授权

US5877221A Compositions containing and methods of using 1-aminoindan and derivatives thereof and process for preparing optically active 1-aminoindan derivatives 失效
标题翻译：包含使用1-氨基茚丹及其衍生物的组合物和制备光学活性1-氨基茚满衍生物的方法
公开(公告)号：US5877221A
公开(公告)日：1999-03-02
申请号：US953097
申请日：1997-10-17
申请人： Sasson Cohen , Yaacov Herzig , Ruth Levy , Jeff Sterling , Alex Veinberg , Moussa B. H. Youdim , John P. M. Finberg
发明人： Sasson Cohen , Yaacov Herzig , Ruth Levy , Jeff Sterling , Alex Veinberg , Moussa B. H. Youdim , John P. M. Finberg
IPC分类号： A01N37/18 , A01N37/34 , A61K31/135 , A61K31/137 , A61K31/16 , A61K31/165 , A61K31/166 , A61K31/167 , A61K31/18 , A61K31/195 , A61K31/196 , A61K31/215 , A61K31/216 , A61K31/24 , A61K31/27 , A61K31/275 , A61K31/277 , C07C209/04 , C07C209/88 , C07C211/00 , C07C211/38 , C07C211/42 , C07C213/10 , C07C215/44 , C07C217/74 , C07C231/20 , C07C233/05 , C07C233/06 , C07C233/23 , C07C233/74 , C07C237/04
CPC分类号： C07C237/04 , A61K31/135 , A61K31/136 , A61K31/137 , A61K31/165 , A61K31/166 , A61K31/167 , A61K31/18 , A61K31/195 , A61K31/196 , A61K31/215 , A61K31/216 , A61K31/24 , A61K31/27 , A61K31/275 , A61K31/277 , C07C209/04 , C07C209/88 , C07C211/38 , C07C211/42 , C07C213/10 , C07C215/44 , C07C217/52 , C07C217/74 , C07C231/20 , C07C233/03 , C07C233/06 , C07C233/11 , C07C233/14 , C07C233/23 , C07C233/52 , C07C233/65 , C07C233/74 , C07C235/54 , C07C237/22 , C07C237/48 , C07C255/24 , C07C255/58 , C07C271/22 , C07C2102/08 , C07C2102/10
摘要： Novel derivatives of 1-aminoindan and their salts are described. Optically active 1-aminoindan derivatives are prepared by reacting a N-benzyl analog of the desired compound with an enantiomer of mandelic acid. Parkinson's disease, dementia, epilepsy, convulsions, or seizures are treated by administering a compound of the formula: ##STR1##
摘要翻译：描述了1-氨基茚满及其盐的新型衍生物。通过使所需化合物的N-苄基类似物与扁桃酸的对映异构体反应来制备光学活性的1-氨基茚满衍生物。帕金森病，痴呆，癫痫，惊厥或癫痫发作通过施用下式化合物治疗：

10. 发明授权

US5684199A Process for the preparation of an optically pure enantiomer of formoterol 失效
标题翻译：制备福莫特罗的光学纯对映异构体的方法
公开(公告)号：US5684199A
公开(公告)日：1997-11-04
申请号：US663143
申请日：1996-06-13
申请人： Eric Francotte
发明人： Eric Francotte
IPC分类号： C07C231/20 , C07C233/43
CPC分类号： C07C233/43 , C07C231/20
摘要： The present invention is directed to a process for preparing formoterol and related compounds and derivatives thereof and their pharmacologically and pharmaceutically acceptable fumarate salts and/or solvates. The present invention is also directed to certain formoterol related compounds per se.
摘要翻译： PCT No.PCT / EP94 / 04199 Sec。 371日期：1996年6月13日 102（e）1996年6月13日PCT 1996年12月16日PCT PCT。 WO95 / 18094 PCT公开号日期1995年7月6日本发明涉及制备福莫特罗及其相关化合物及其衍生物及其药理学和药学上可接受的延胡索酸盐和/或溶剂合物的方法。本发明还涉及某些福莫特罗相关化合物本身。

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