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21. 发明申请

US20180029975A1 SYNTHESIS PROCESS FOR CHIRAL CYCLOPROPYL ETHYNYL TERTIARY ALCOHOL COMPOUND 审中-公开
公开(公告)号：US20180029975A1
公开(公告)日：2018-02-01
申请号：US15551142
申请日：2015-10-23
申请人： Shanghai Desano Pharmaceutical Co., Ltd. , Yancheng Desano Pharmaceutical Co., Ltd. , Jiangsu Puxin Pharmaceutical Co., Ltd.
发明人： Nan ZHAO , Fei JIANG
IPC分类号： C07C213/10 , C07C213/00 , C07B53/00
CPC分类号： C07C213/10 , C07B53/00 , C07B2200/07 , C07C213/00 , C07C215/70 , C07C2601/02 , C07D265/18
摘要： Provided is a synthesis process for a chiral cyclopropyl ethynyl tertiary alcohol compound, where a chiral amino alcohol or a chiral amino diol is reacted in the presence of an alkaline reagent and a salt to obtain an optically active propynyl alcohol compound. In particular, the process includes (1) reacting cyclopropyl acetylene with a chiral inducing agent, a chiral auxiliary reagent and zinc halide in an organic solvent in the presence of an alkaline reagent and a sulfonate or a sulphinate to obtain a first reaction mixture; (2) reacting the resultant first reaction mixture with 5-chloro-2-aminotrifluorobenzophenone to form (S)-2-amino-5-chloro-α-cyclopropyl acetylene-α-trifluoromethylbenzyl alcohol. The process avoids an organic zinc reagent and a Grignard reagent, and has the advantages of safe production, an environmentally friendly route, low production costs, a high resultant product yield, a high chiral ee value and is suitable for industrial production.

22. 发明申请

US20170158608A1 Process for the Preparation of 2-Alkoxymethyl-1,4-Benzenediamines 审中-公开
公开(公告)号：US20170158608A1
公开(公告)日：2017-06-08
申请号：US15260524
申请日：2016-09-09
申请人： The Procter & Gamble Company
发明人： Bryan Patrick MURPHY , Garry Steven GARRETT , John Michael GARDLIK
IPC分类号： C07C213/10 , C07C209/74 , A61K8/41 , C07C213/08 , C07D207/404 , A61Q5/10 , C07C209/68 , C07C213/00
CPC分类号： A61K8/411 , A61Q5/10 , C07C209/74 , C07C213/00 , C07C213/02 , C07D207/404 , C07D209/48 , C07C211/52 , C07C217/76
摘要： A process for synthesizing 2-methoxymethyl-1,4-benzenediamine (V-a), its derivatives of formula (V) and the salts thereof, which comprises a radical halogenation step of formula (II). The final product can be 2-methoxymethyl-1,4-benzenediamine of formula (IV-a).

23. 发明授权

US09586883B2 Aldehyde-selective wacker-type oxidation of unbiased alkenes 有权
标题翻译：醛类选择性瓦克型氧化无偏烯烃
公开(公告)号：US09586883B2
公开(公告)日：2017-03-07
申请号：US14255049
申请日：2014-04-17
申请人： CALIFORNIA INSTITUTE OF TECHNOLOGY
发明人： Zachary K. Wickens , Bill Morandi , Robert H. Grubbs , Kacper Skakuj , Sarah M. Bronner
IPC分类号： C07C45/34 , C07C249/04 , C07C253/00 , C07C201/12 , C07C205/44 , C07C209/60 , C07C213/00 , C07C227/08 , C07C51/373 , C07C59/235 , C07C211/48 , C07C217/48 , C07D301/22
CPC分类号： C07C45/34 , C07C51/373 , C07C201/12 , C07C205/44 , C07C209/60 , C07C213/00 , C07C227/08 , C07C249/04 , C07C253/00 , C07D301/22 , C07C59/235 , C07C211/48 , C07C217/48 , C07C229/18 , C07C47/02 , C07C47/11 , C07C47/14 , C07C47/19 , C07C47/198 , C07C47/277
摘要： This disclosure is directed to methods of preparing organic aldehydes, each method comprising contacting a terminal olefin with an oxidizing mixture comprising: (a) a dichloro-palladium complex; (b) a copper complex; (c) a source of nitrite; under aerobic reaction conditions sufficient to convert at least a portion of the terminal olefin to an aldehyde.
摘要翻译：本公开涉及制备有机醛的方法，每种方法包括使末端烯烃与氧化混合物接触，所述氧化混合物包含：（a）二氯 - 钯络合物; （b）铜络合物; （c）亚硝酸盐源; 在需氧反应条件下，足以将至少一部分末端烯烃转化为醛。

24. 发明授权

US09580616B2 Dispersants 有权
标题翻译：分散剂
公开(公告)号：US09580616B2
公开(公告)日：2017-02-28
申请号：US13984711
申请日：2012-02-06
申请人： Dario Fornara , Alan Nappa , Tamara Verzotti , Paolo Prampolini , Stefano Crespi , Giovanni Floridi , Giuseppe Li Bassi
发明人： Dario Fornara , Alan Nappa , Tamara Verzotti , Paolo Prampolini , Stefano Crespi , Giovanni Floridi , Giuseppe Li Bassi
IPC分类号： C08K5/15 , C07C211/00 , B32B7/12 , C09D11/00 , C07D295/18 , C07C53/00 , C07C213/00 , C07C217/00 , C09D11/38 , C04B41/00 , C04B41/45 , C04B41/81 , C08G73/02 , C09D11/326 , C09D7/02 , C08L79/02
CPC分类号： C09D11/38 , C04B41/009 , C04B41/4539 , C04B41/81 , C08G73/024 , C08L79/02 , C09D7/45 , C09D11/326 , C04B33/00 , C04B2103/408 , C04B2103/54
摘要： Compound of Formula (1); wherein: Zw is an organic radical comprising w amino groups, in which w is a number and 5≦w≦3,000; A and B are independently oxy-C1-C20-alkylene carbonyl groups or oxy-C2-C20-alkenylene carbonyl groups derived from hydroxy carboxylic acids or lactones; T is hydrogen or R—CO—, where R is a C1-C50 hydrocarbyl group; Y is a C3-C4-alkylene radical linked to an amino group of Zw; Y′ is an ionic salt link between an amino group of Zw and the terminal carbonyl of (A)r-(B)p-T; r and p are independently numbers between 0 and 50 and r+p>2; s, m and v are numbers; 0.99w≦s+m≦2w; and 0.3w≦s+v≦2w are suitable as dispersants and milling aids.
摘要翻译：式（1）的化合物; 其中：Zw是包含w个氨基的有机基团，其中w是数，5≤b≤3000; A和B独立地为羟基-C 1 -C 20亚烷基羰基或衍生自羟基羧酸或内酯的氧-C2-C20亚烯基羰基; T是氢或R-CO-，其中R是C1-C50烃基; Y是与Zw的氨基连接的C3-C4-亚烷基; Y'是Zw的氨基与（A）r-（B）p-T的末端羰基之间的离子盐连接; r和p分别是0和50之间的数字，r + p> 2; s，m和v是数字; 0.99w @ s + m @ 2w; 和0.3w @ s + v @ 2w适合作为分散剂和研磨助剂。

25. 发明申请

US20160368857A1 (HETERO)ARYL CYCLOPROPYLAMINE COMPOUNDS AS LSD1 INHIBITORS 审中-公开
公开(公告)号：US20160368857A1
公开(公告)日：2016-12-22
申请号：US15254020
申请日：2016-09-01
申请人： Oryzon Genomics S.A.
发明人： Alberto ORTEGA MUÑOZ , Matthew Colin Thor FYFE , Marc MARTINELL PEDEMONTE , Maria de los Àngeles ESTIARTE MARTINEZ , Nuria VALLS VIDAL , Guido KURZ , Julio Cesar CASTRO PALOMINO LARIA
IPC分类号： C07C211/36 , C07D277/28 , C07D213/38 , C07C217/74 , C07C213/00 , C07D207/14 , C07C211/38 , C07C271/24 , C07C269/00 , C07C275/26 , C07C273/00 , C07D295/135 , C07C215/64 , C07D231/56 , C07D231/12 , C07D333/20 , C07D213/57 , C07D213/73 , C07D295/26 , C07D295/096 , C07D213/30 , C07D213/74 , C07C209/28
CPC分类号： C07C211/36 , C07B2200/07 , C07C209/28 , C07C211/37 , C07C211/38 , C07C211/40 , C07C213/00 , C07C215/46 , C07C215/64 , C07C217/54 , C07C217/74 , C07C269/00 , C07C271/24 , C07C273/00 , C07C273/18 , C07C275/26 , C07C311/08 , C07C311/21 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07C2602/08 , C07D207/14 , C07D213/30 , C07D213/38 , C07D213/57 , C07D213/73 , C07D213/74 , C07D231/12 , C07D231/56 , C07D277/28 , C07D295/096 , C07D295/135 , C07D295/26 , C07D307/52 , C07D333/20
摘要： The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.

26. 发明授权

US09447067B2 Method of preparing intermediate of salmeterol 有权
标题翻译：制备沙美特罗中间体的方法
公开(公告)号：US09447067B2
公开(公告)日：2016-09-20
申请号：US14714196
申请日：2015-05-15
申请人： AMPHASTAR PHARMACEUTICALS INC.
发明人： Yinhua Qiu , Zhengyuan Wu , Song Chen , Haoning Zhang
IPC分类号： C07D319/08 , C07C213/00
CPC分类号： C07D319/08 , C07C213/00
摘要： A method of preparing an intermediate of salmeterol (Compound 1, 2-amino-1-(2,2-dimethyl-4H-1,3-benzodioxin-6-yl)ethanol) includes: reacting compound 2 with 2-methoxypropene in a first organic solvent to produce a reaction solution including compound 3, compound 2 including a 2-bromo precursor of Compound 1; reacting compound 3 with a nitrogen source to produce compound 4; reacting compound 4 with sodium borohydride in a second organic solvent to produce compound 5; and debenzylating compound 5 by ammonium formate/palladium-carbon catalytic transfer hydrogenation in a third organic solvent to produce Compound 1. A method of preparing salmeterol includes preparing Compound 1, and reacting Compound 1 to prepare salmeterol.
摘要翻译：制备沙美特罗（化合物1,2,2-氨基-1-（2,2-二甲基-4H-1,3-苯并二恶英-6-基）乙醇）的中间体的方法包括：使化合物2与2-甲氧基丙烯反应第一有机溶剂以产生包括化合物3，包含化合物1的2-溴前体的化合物2的反应溶液; 使化合物3与氮源反应生成化合物4; 使化合物4与硼氢化钠在第二有机溶剂中反应生成化合物5; 和在第三有机溶剂中通过甲酸铵/钯 - 碳催化转移氢化脱苄化化合物5以制备化合物1.制备沙美特罗的方法包括制备化合物1，并使化合物1与制备沙美特罗进行反应。

27. 发明授权

US09421532B2 Mononuclear iron complex and organic synthesis reaction using same 有权
标题翻译：单核铁络合物与有机合成反应使用相同
公开(公告)号：US09421532B2
公开(公告)日：2016-08-23
申请号：US14771757
申请日：2014-02-26
申请人： KYUSHU UNIVERSITY, NATIONAL UNIVERSITY CORPORATION , SHIN-ETSU CHEMICAL CO., LTD.
发明人： Hideo Nagashima , Yusuke Sunada , Hironori Tsutsumi , Toru Hashimoto , Koji Sakuta
IPC分类号： B01J31/16 , C07F15/02 , C07D223/04 , C07C5/03 , C07C29/147 , C07C41/26 , C07C209/50 , B01J31/20 , B01J31/22 , C07C213/02 , C07C227/16 , C07C227/18 , C07C29/14 , C07F7/08 , C07C41/18 , C07C213/00 , C07C227/06
CPC分类号： B01J31/1608 , B01J31/20 , B01J31/226 , B01J2231/323 , B01J2231/643 , B01J2231/645 , B01J2531/842 , C07C5/03 , C07C29/14 , C07C29/147 , C07C41/18 , C07C41/26 , C07C209/50 , C07C213/00 , C07C213/02 , C07C227/06 , C07C227/16 , C07C227/18 , C07C2531/16 , C07C2531/20 , C07C2531/22 , C07C2601/08 , C07C2601/14 , C07D223/04 , C07F7/0805 , C07F7/0829 , C07F15/02 , Y02P20/52 , C07C43/23 , C07C9/16 , C07C13/18 , C07C13/10 , C07C15/073 , C07C15/18 , C07C211/29 , C07C211/27 , C07C217/58 , C07C229/38 , C07C33/20 , C07C31/1355
摘要： Provided is a mononuclear iron complex that comprises an iron-silicon bond that is represented by formula (1) and that exhibits excellent catalyst activity in each of a hydrosilylation reaction, a hydrogenation reaction, and reduction of a carbonyl compound. In formula (1), R1-R6 either independently represent an alkyl group, an aryl group, an aralkyl group or the like that may be substituted with a hydrogen atom or X, or represent a crosslinking substituent in which at least one pair comprising one of R1-R3 and one of R4-R6 is combined. X represents a halogen atom, an organoxy group, or the like. L represents a two-electron ligand other than CO. When a plurality of L are present, the plurality of L may be the same as or different from each other. When two L are present, the two L may be bonded to each other. n and m independently represent an integer of 1 to 3 with the stipulation that n+m equals 3 or 4.
摘要翻译：提供一种单核铁配合物，其包含由式（1）表示的铁 - 硅键，并且在氢化硅烷化反应，氢化反应和羰基化合物的还原中显示出优异的催化剂活性。在式（1）中，R 1 -R 6独立地表示可以被氢原子或X取代的烷基，芳基，芳烷基等，或者表示交联取代基，其中至少一个包含一个的R1-R3和R4-R6之一组合。 X表示卤素原子，有机氧基等。 L表示除CO以外的双电子配体，当存在多个L时，多个L可以彼此相同或不同。当存在两个L时，两个L可以彼此结合。 n和m独立地表示1〜3的整数，其中n + m等于3或4。

28. 发明授权

US09359279B2 Treatment of cancer, inflammatory disease, and autoimmune disease 有权
标题翻译：治疗癌症，炎性疾病和自身免疫性疾病
公开(公告)号：US09359279B2
公开(公告)日：2016-06-07
申请号：US14471539
申请日：2014-08-28
申请人： AndroScience Corporation
发明人： Charles C-Y Shih , Toshio Kitamura , Qian Shi , Toshiyuki Kawashima , Hui-Kang Wang
IPC分类号： C07D211/20 , C07C49/00 , C07C307/00 , C07C309/00 , C07C303/00 , C07C311/00 , C07F9/02 , C07C233/00 , C07C235/00 , C07C237/00 , C07C239/00 , C07C213/00 , C07C215/00 , C07C217/00 , A61K31/66 , A61K31/12 , A61K31/255 , A61K31/445 , A61K31/165 , A61K31/135 , A61K31/535 , C07C49/248 , C07C49/235 , C07C49/255 , C07C69/16 , C07C217/22 , C07C235/82 , C07C307/02 , C07C309/65 , C07C309/66 , C07C309/73 , C07C317/24 , C07D213/68 , C07D295/112 , C07F9/12 , C07F9/32 , C07C217/60 , C07D295/13 , C07F9/06 , C07F9/09
CPC分类号： C07C49/248 , C07C49/235 , C07C49/255 , C07C69/16 , C07C217/22 , C07C217/60 , C07C235/82 , C07C307/02 , C07C309/65 , C07C309/66 , C07C309/73 , C07C317/24 , C07C2601/14 , C07C2601/16 , C07D213/68 , C07D295/112 , C07D295/13 , C07F9/06 , C07F9/09 , C07F9/12 , C07F9/32 , C07F9/3282
摘要： A method of treating cancer, inflammatory disease, and autoimmune disease by administering to a subject in need thereof an effective amount of one or more 1,5-dipenylpenta-1,4-dien-3-one compounds. The compounds feature either or both of the phenyl rings being substituted with hydroxyl, diethyl(2-alkoxyethyl)amine, 1-(2-alkoxyethyl)piperidine, sulfonate, phosphinate, or phosphate.
摘要翻译：一种通过向有需要的受试者施用有效量的一种或多种1,5-二烯基戊-1,4-二烯-3-酮化合物来治疗癌症，炎性疾病和自身免疫性疾病的方法。这些化合物的特征在于一个或两个苯环被羟基，二乙基（2-烷氧基乙基）胺，1-（2-烷氧基乙基）哌啶，磺酸盐，次膦酸盐或磷酸盐取代。

29. 发明申请

US20160096816A1 METHOD OF PREPARING INTERMEDIATE OF SALMETEROL 有权
标题翻译：制备沙利度醇中间体的方法
公开(公告)号：US20160096816A1
公开(公告)日：2016-04-07
申请号：US14714196
申请日：2015-05-15
申请人： AMPHASTAR PHARMACEUTICALS INC.
发明人： Yinhua Qiu , Zhengyuan Wu , Song Chen , Haoning Zhang
IPC分类号： C07D319/08 , C07C213/00
CPC分类号： C07D319/08 , C07C213/00
摘要： A method of preparing an intermediate of salmeterol (Compound 1, 2-amino-1-(2,2-dimethyl-4H-1,3-benzodioxin-6-yl)ethanol) includes: reacting compound 2 with 2-methoxypropene in a first organic solvent to produce a reaction solution including compound 3, compound 2 including a 2-bromo precursor of Compound 1; reacting compound 3 with a nitrogen source to produce compound 4; reacting compound 4 with sodium borohydride in a second organic solvent to produce compound 5; and debenzylating compound 5 by ammonium formate/palladium-carbon catalytic transfer hydrogenation in a third organic solvent to produce Compound 1. A method of preparing salmeterol includes preparing Compound 1, and reacting Compound 1 to prepare salmeterol.
摘要翻译：制备沙美特罗（化合物1,2,2-氨基-1-（2,2-二甲基-4H-1,3-苯并二恶英-6-基）乙醇）的中间体的方法包括：使化合物2与2-甲氧基丙烯反应第一有机溶剂以产生包括化合物3，包含化合物1的2-溴前体的化合物2的反应溶液; 使化合物3与氮源反应生成化合物4; 使化合物4与硼氢化钠在第二有机溶剂中反应生成化合物5; 和在第三有机溶剂中通过甲酸铵/钯 - 碳催化转移氢化脱苄化化合物5以制备化合物1.制备沙美特罗的方法包括制备化合物1，并使化合物1与制备沙美特罗进行反应。

30. 发明授权

US09216944B2 Process for the production of choline hydroxide 有权
标题翻译：生产氢氧化胆碱的方法
公开(公告)号：US09216944B2
公开(公告)日：2015-12-22
申请号：US14369014
申请日：2011-12-29
申请人： Kristof Moonen , Dieter Ulrichts , Daan Scheldeman
发明人： Kristof Moonen , Dieter Ulrichts , Daan Scheldeman
IPC分类号： C07C213/00 , C07C215/00 , C07C217/00 , C07C213/10 , C07C213/04
CPC分类号： C07C213/10 , C07C213/04 , C07C215/40
摘要： A continuous process for the production of choline hydroxide includes reacting ethylene oxide, trimethylamine, and water in a reaction zone to form a reaction mixture and extracting heat from the reaction mixture. Subsequently, phase separation of the reaction mixture is induced to obtain a choline hydroxide phase and an organic liquid phase comprising trimethylamine. A choline hydroxide solution (e.g., at a concentration of about 40% to 50% by weight, based on total weight of the choline hydroxide solution) is obtained from the choline hydroxide phase.
摘要翻译：用于生产氢氧化胆碱的连续方法包括在反应区中使环氧乙烷，三甲胺和水反应以形成反应混合物并从反应混合物中提取热量。随后，诱导反应混合物的相分离，得到含有三甲胺的氢氧化胆碱相和有机液相。从氢氧化胆碱相获得氢氧化胆碱溶液（例如浓度为约40％至50％重量，基于氢氧化胆碱溶液的总重量）。

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