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1. 发明申请

WO2014172042A1 SYNTHESIS OF NOVEL IONIC LIQUIDS FROM LIGNIN-DERIVED COMPOUNDS 审中-公开
标题翻译：来自LIGNIN衍生化合物的新型离子液体的合成
公开(公告)号：WO2014172042A1
公开(公告)日：2014-10-23
申请号：PCT/US2014/028684
申请日：2014-03-14
申请人： SANDIA CORPORATION , THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
发明人： SOCHA, Aaron , SINGH, Seema , SIMMONS, Blake A. , BERGERON, Maxime
IPC分类号： C07C211/01 , B01F1/00
CPC分类号： C07D307/52 , C07C209/00 , C07C209/04 , C07C209/28 , C07C211/28 , C07C211/63 , C07C213/02 , C07C213/08 , C07C215/66 , C07C217/58 , C07D295/03 , C08H8/00 , C09K3/00 , C12P19/02 , C12P19/14 , H01M10/0569 , H01M2300/0037 , H01M2300/0045 , C07C215/50 , C07C211/27
摘要： Methods and compositions are provided for synthesizing ionic liquids from lignin derived compounds comprising: contacting a starting material comprising lignin with a depolymerization agent to depolymerize the lignin and form a mixture of aldehyde containing compounds; contacting the mixture of aldehyde containing compounds with an amine under conditions suitable to convert the mixture of aldehyde containing compounds to a mixture of amine containing compounds; and contacting the mixture of amine containing compounds with an acid under conditions suitable to form an ammonium salt, thereby preparing the ionic liquid.
摘要翻译：提供了用于从木质素衍生的化合物合成离子液体的方法和组合物，包括：使包含木质素的原料与解聚剂接触以使木质素解聚并形成含醛化合物的混合物; 在适于将含醛化合物的混合物转化为含胺化合物的混合物的条件下，使含醛化合物的混合物与胺接触; 并在适于形成铵盐的条件下使含胺化合物的混合物与酸接触，由此制备离子液体。

2. 发明申请

WO2009153814A1 A PROCESS FOR THE SYNTHESIS OF CINACALCET HYDROCHLORIDE 审中-公开
标题翻译： CINACALCET HYDROCHLORIDE的合成方法
公开(公告)号：WO2009153814A1
公开(公告)日：2009-12-23
申请号：PCT/IT2008/000404
申请日：2008-06-18
申请人： ERREGIERRE S.p.A. , FERRARI, Massimo , GHEZZI, Marcello , BONALDI, Matteo
发明人： FERRARI, Massimo , GHEZZI, Marcello , BONALDI, Matteo
IPC分类号： C07C209/28 , C07C211/30
CPC分类号： C07C209/28 , C07C211/30
摘要： There is described a process for the preparation of cinacalcet hydrochloride (I) which includes the steps of: a) reacting (R)-(+)-1-(1-naphthyl)ethylamine (II) with 3-[3-(trifluoromethyl)phenyl]propenaldehyde (III) to afford the non isolated intermediate (R)-N-[3-[3-(trifluoromethyl)phenyl]-2-propenylimino-N-[1-(1 - naphthyi)ethy!amine (IV); b) reducing the non isolated intermediate (R)-N-[3-[3-(trifluoromethyl)phenyl]-2-propenylimine-N-[-1 -(1 -naphthyl)ethylamine (IV) with a sequential addition of: - a solution of sodium borohydride, methanol and a base, - oxalic acid and - a base to obtain (R)-N-[3-[3-(trifluoromethyl)phenyl]-2- propenyl]-1-(1-naphthyl)ethylamine (V) by passing through the precipitation of the oxalate salt of compound (V) after the addition of oxalic acid; c) hydrogenating (R)-N-[3-[3-(trifluoromethyl)phenyl]-2-propenyl]-1 -(1 - naphthyl)ethylamine (V) thus obtaining (R)-N-(3-(3- (trifluoromethyl)phenyl]propyij-i-(i -naphthyl)ethylamine cinacalcet base (Vl), which is retaken in ethyl acetate; and d) treating the- solution of cinacalcet base (Vi) in ethyl acetate with hydrochloric acid to afford cinacalcet hydrochloride (I).
摘要翻译：描述了制备西那卡塞盐酸盐（I）的方法，其包括以下步骤：a）使（R） - （+） - 1-（1-萘基）乙胺（II）与3- [3-（三氟甲基））苯基]丙醛（III），得到非分离的中间体（R）-N- [3- [3-（三氟甲基）苯基] -2-丙烯基亚氨基-N- [1-（1-萘基）乙基胺（IV ）; b）依次加入非离子中间体（R）-N- [3- [3-（三氟甲基）苯基] -2-丙烯基亚胺-N - [1-（1-萘基）乙胺（IV））， - 硼氢化钠，甲醇和碱的溶液 - 草酸和碱，得到（R）-N- [3- [3-（三氟甲基）苯基] -2-丙烯基] -1-（1-萘基）乙胺（V）通过在加入草酸后通过化合物（V）的草酸盐的沉淀; c）氢化（R）-N- [3- [3-（三氟甲基）苯基] -2-丙烯基] -1-（1-萘基）乙胺（V），由此得到（R）-N-（3-（3 - （三氟甲基）苯基]丙基] - （1-萘基）乙胺西那卡塞碱（VI），其在乙酸乙酯中再次;和d）用盐酸将西那卡赛碱（Vi）溶液在乙酸乙酯中处理，得到盐酸西那卡塞（I）。

3. 发明申请

WO2008068625A2 PROCESSES FOR PREPARING CINACALCET HYDROCHLORIDE AND POLYMORPHIC FORMS THEREOF 审中-公开
标题翻译：制备CINACALCET HYDROCHLORIDE的方法及其多晶型
公开(公告)号：WO2008068625A2
公开(公告)日：2008-06-12
申请号：PCT/IB2007004309
申请日：2007-06-08
申请人： MEDICHEM SA , SZEKERES TIBOR , REPASI JOZSEF , SZABO ANDRAS , BENITO VELEZ MONICA , MANGION BERNARDINO
发明人： SZEKERES TIBOR , REPASI JOZSEF , SZABO ANDRAS , BENITO VELEZ MONICA , MANGION BERNARDINO
IPC分类号： C07C209/28 , C07C209/84 , C07C211/30
CPC分类号： C07C209/84 , C07B2200/13 , C07C209/28 , C07C211/30
摘要： The invention relates to cinacalcet hydrochloride, new polymorphic crystalline forms of cinacalcet hydrochloride, amorphous cinacalcet hydrochloride and synthetic processes for their preparation.
摘要翻译：本发明涉及盐酸西那卡塞，盐酸西那卡塞的新型多晶型物，盐酸无定形西那卡塞及其制备方法。

4. 发明申请

WO2006134224A1 CONTROLLING THE REGIO- AND STEREOSPECIFICITY OF ENZYME CATALYSIS WITH GUIDE MOLECULES 审中-公开
标题翻译：用指南分子控制酶的催化分解和立体定向
公开(公告)号：WO2006134224A1
公开(公告)日：2006-12-21
申请号：PCT/FI2006/050248
申请日：2006-06-09
申请人： KEINÄNEN, Tuomo , JÄRVINEN, Aki , VEPSÄLÄINEN, Jouko , UIMARI, Anne , ALHONEN, Leena , JÄNNE, Juhani
发明人： KEINÄNEN, Tuomo , JÄRVINEN, Aki , VEPSÄLÄINEN, Jouko , UIMARI, Anne , ALHONEN, Leena , JÄNNE, Juhani
IPC分类号： C12P13/00 , C12P1/00 , C12P41/00 , C07C211/14 , C07D213/69
CPC分类号： C07C209/28 , C12P13/001 , C12P41/00 , C07C211/14
摘要： The present invention is directed to methods for controlling regiospecificity and stereospecificity of enzyme catalysis with guide molecules. The use of guide molecules in biocatalysis of different kind of chiral or achiral chemicals allows the production of chemicals with predetermined chiral/chemical structure. Guide molecules can be used to destroy undesired isomers among the racemic precursor molecules (leaving the target isomer intact) or to produce selected precursor molecules by enzymatic cleavage of the guide molecule activated isomer in the racemic reaction mixture. Guide molecules may be used for controlling drug metabolism in humans/non-humans and also for preparing novel prodrugs.
摘要翻译：本发明涉及用引导分子控制酶催化的区域特异性和立体定向性的方法。在不同种类的手性或非手性化学品的生物催化中使用指导分子允许生产具有预定手性/化学结构的化学品。引导分子可以用于消除外消旋前体分子（留下目标异构体完整）中的不需要的异构体，或通过外消旋反应混合物中的引导分子活化异构体的酶切割产生选定的前体分子。引导分子可用于控制人/非人类中的药物代谢，也可用于制备新的前药。

5. 发明申请

WO2005121074A2 PROCESSES FOR THE PREPARATION OF SERTRALINE HYDROCHLORIDE 审中-公开
标题翻译：制备盐酸氯化物的方法
公开(公告)号：WO2005121074A2
公开(公告)日：2005-12-22
申请号：PCT/IB2005051911
申请日：2005-06-09
申请人： RANBAXY LAB LTD , RAMANA KINTALI VENKATA , SINGH KAPTAN , PRASAD MOHAN , DEO KESHAV , KUMAR YATENDRA
发明人： RAMANA KINTALI VENKATA , SINGH KAPTAN , PRASAD MOHAN , DEO KESHAV , KUMAR YATENDRA
IPC分类号： A61K31/135 , C07C209/26 , C07C209/28 , C07C209/44 , C07C209/88 , C07C211/42 , C07C249/02 , C07C251/20 , C07C249/00
CPC分类号： C07C249/02 , C07C209/28 , C07C209/44 , C07C211/42 , C07C251/20
摘要： The invention relates to processes for the preparation of Schiff's base, and to the use of Schiff's base as intermediate in the preparation of naphthalenamine derivatives which are active compounds for treating the anxiety related disorders. The invention also relates to processes for the preparation of sertraline or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions that include the sertraline.
摘要翻译：本发明涉及席夫碱的制备方法，以及席夫碱的制备中用于制备作为治疗焦虑症的活性化合物的萘胺衍生物的方法。本发明还涉及制备舍曲林或其药学上可接受的盐的方法，以及包括舍曲林的药物组合物。

6. 发明申请

WO2014135508A1 VERFAHREN ZUR HERSTELLUNG VON HALOGEN-N,N-DIMETHYLBENZYLAMINEN 审中-公开
标题翻译：用于生产卤N，DIMETHYLBENZYLAMINEN
公开(公告)号：WO2014135508A1
公开(公告)日：2014-09-12
申请号：PCT/EP2014/054108
申请日：2014-03-04
申请人： LANXESS DEUTSCHLAND GMBH
发明人： PETERS, Lars , SCHULZE TILLING, Andreas , STIRNER, Wolfgang
IPC分类号： C07C209/26 , C07C211/29
CPC分类号： C07C209/28 , C07C209/26 , C07C211/29
摘要： Die Erfindung betrifft ein Verfahren zur Herstellung von Halogen-N,N- dimethylbenzylaminenmit Halogen = Chlor oder Brom, vorzugsweise Chlor-N,N- dimethylbenzylaminen, vorzugsweise ortho-Chlor-N,N-dimethylbenzylamin (o-Cl-DMBA), durch reduktive Aminierung in Abwesenheit von Schwefel.
摘要翻译：本发明涉及用于卤-N的制备方法，N- dimethylbenzylaminenmit卤素是（邻CL-DMBA）通过还原氯或溴，优选氯-N，N- dimethylbenzylaminen，优选邻 - 氯-N，N-二甲基苄胺化在不存在硫。

7. 发明申请

WO2010041964A1 METHODS FOR THE PREPARATION OF ALKENYLAMINES, CYCLIC CARBAMATES OR DITHIOCARBAMATES, AND AMINOALCOHOLS OR AMINOTHIOLS 审中-公开
标题翻译：制备亚苄基胺，环状碳酸酯或二烷基甲酸酯的方法，以及氨基醇或氨基酸
公开(公告)号：WO2010041964A1
公开(公告)日：2010-04-15
申请号：PCT/NZ2009/000216
申请日：2009-10-09
申请人： VICTORIA LINK LIMITED , DANGERFIELD, Emma, M. , STOCKER, Bridget, L. , TIMMER, Mattheus, S., M.
发明人： DANGERFIELD, Emma, M. , STOCKER, Bridget, L. , TIMMER, Mattheus, S., M.
IPC分类号： C07D498/04 , C07C215/24 , C07C209/28 , C07D207/12
CPC分类号： C07D207/12 , C07C209/28 , C07C215/24 , C07D498/04
摘要： A method for preparing an alkenylamine, or a salt, solvate or hydrate thereof, is disclosed. The method comprises reacting a alogen-substituted cyclic acetal or a derivative thereof under particular conditions to provide the alkenylamine, which may be optionally converted into a salt, solvate or hydrate thereof. A method for preparing a cyclic carbamate or cyclic dithiocarbamate, or a salt, solvate or hydrate thereof, is also disclosed. The method comprises reacting an alkenylamine under particular conditions to provide the cyclic carbamate or cyclic dithiocarbamate, which may be optionally converted into a salt, solvate or hydrate thereof. A method for preparing a 1,2-aminoalcohol or 1,2-aminothiol, or a salt, solvate or hydrate thereof, is also disclosed. The method comprises forming a cyclic carbamate or cyclic dithiocarbamate from an alkenylamine, and deprotecting the cyclic carbamate or cyclic dithiocarbamate to provide the 1,2-aminoalcohol or 1,2-aminothiol, which may optionally be converted into a salt, solvate or hydrate thereof.
摘要翻译：公开了一种制备链烯基胺或其盐，溶剂合物或水合物的方法。该方法包括在特定条件下使一个取代的环缩醛或其衍生物与可以任选地转化为其盐，溶剂化物或水合物的链烯基胺反应。还公开了环状氨基甲酸酯或环状二硫代氨基甲酸盐或其盐，溶剂合物或水合物的制备方法。该方法包括在特定条件下使烯基胺反应以提供环状氨基甲酸酯或环状二硫代氨基甲酸酯，其可以任选地转化成其盐，溶剂合物或水合物。还公开了制备1,2-氨基醇或1,2-氨基硫醇或其盐，溶剂化物或水合物的方法。该方法包括由烯基胺形成环状氨基甲酸酯或环状二硫代氨基甲酸酯，并使环状氨基甲酸酯或环状二硫代氨基甲酸酯脱保护，得到1,2-氨基醇或1,2-氨基硫醇，其可以任选地转化为其盐，溶剂合物或水合物。

8. 发明申请

WO2006008171A1 PROCESS FOR THE PREPARATION OF A DIASTEREOMERICALLY ENRICHED COMPOUND 审中-公开
标题翻译：制备二异氰酸酯化合物的方法
公开(公告)号：WO2006008171A1
公开(公告)日：2006-01-26
申请号：PCT/EP2005/007988
申请日：2005-07-20
申请人： DSM IP ASSETS B.V. , BROXTERMAN, Quirinus, Bernardus , LANGE, De Ben , ELSENBERG, Henricus, Leonardus, Marie , WEBER, Matthias
发明人： BROXTERMAN, Quirinus, Bernardus , LANGE, De Ben , ELSENBERG, Henricus, Leonardus, Marie , WEBER, Matthias
IPC分类号： C07C211/27
CPC分类号： C07C209/28 , C07C2601/02 , C07C211/17 , C07C211/27 , C07C211/29
摘要： The present invention relates to a process for the preparation of a diastereomerically enriched compound, wherein a first compound according to formula (I), is contacted with a second compound according to formula (II), to form a third compound according to formula (III), whereby the compound according to formula (III) is subsequently reduced and thereby converted into a compound according to formula (IV), in which formulas: R 1 = a cycloalkylgroup whereby R 1 # R 2 , R 2 = a substituted or unsubstituted: (cyclo)alkyl group, (cyclo)alkenylgroup, aryl group, cyclic or acyclic heteroalkylgroup or heteroarylgroup, R 3 = an alkyl group, R 4 = a substituted or unsubstituted: phenyl- or naphthyl-group, *= a chiral center. The invention furthermore relates to a diastereomerically enriched compound according to formula (IV) and its use in the preparation of pharmaceutical and agrochemically active compounds. The invention further relates to a process for the preparation of enantiomerically enriched compounds of formula (V), through hydrogenolysis of diastereomerically enriched compounds of formula (IV), wherein R 1 and R 2 have the meanings given above.
摘要翻译：本发明涉及一种制备非对映体富集的化合物的方法，其中根据式（I）的第一化合物与式（II）的第二化合物接触，以形成式（III）的第三化合物），由此将式（III）化合物随后还原，由此转化为式（Ⅳ）化合物，其中式

9. 发明申请

WO02051792A1 METHOD FOR THE PRODUCTION OF 1,5-NAPHTHALENEDIAMINE 审中-公开
标题翻译：用于生产1,5-萘二胺
公开(公告)号：WO02051792A1
公开(公告)日：2002-07-04
申请号：PCT/EP2001/014449
申请日：2001-12-10
IPC分类号： C07C209/36 , C07B61/00 , C07C205/45 , C07C209/60 , C07C209/70 , C07C211/37 , C07C211/52 , C07C211/57 , C07C211/60 , C07C233/11 , C07C233/12 , C07C251/20 , C07C253/30 , C07C255/10 , C07C255/42 , C07C265/14 , C07C271/28 , C07C211/45 , C07C211/58
CPC分类号： C07C251/20 , C07C201/12 , C07C205/45 , C07C209/28 , C07C209/36 , C07C209/48 , C07C209/60 , C07C209/68 , C07C211/60 , C07C221/00 , C07C233/11 , C07C249/02 , C07C253/30 , C07C255/42 , C07C2602/10 , C07C225/22 , C07C211/58 , C07C255/35 , C07C211/48
摘要： The invention relates to a method for the production of 1,5-naphthalenediamine and the intermediates obtained in the course of said synthesis, 4-(2-nitrophenyl)-butyronitrile, 5-nitro-3,4-dihydro-1(2H)-naphthylimine, 5-nitroso-1-naphthylamine, 5-nitro-1-naphthylamine, 4-(2-aminophenyl)-butyronitrile, 5-amino-3,4-dihydro-1(2H)-naphthalenimine, ethyl 4-(2-nitrophenyl)-butyrate and 4-(2-nitrophenyl)-butyramide.
摘要翻译：本发明涉及一种方法，代替4-（2-硝基苯基）丁腈，5-硝基-3,4-二氢-1（2H）-naphthylimin，5-的方法期间产生1,5-萘二胺，以及中间产物亚硝基-1-萘基胺，5-硝基-1-萘基胺，4-（2-氨基苯基）丁腈，5-氨基-3,4-二氢-1（2H）-naphthalinimin，4-（2-硝基苯基）丁酸甲酯和4-（2-硝基苯基）-buttersäureamid。

10. 发明申请

WO99058475A2 PREPARATION OF COMPOUNDS USING POLYMER SUPPORTED REAGENTS 审中-公开
标题翻译：使用聚合物支持的试剂制备化合物
公开(公告)号：WO99058475A2
公开(公告)日：1999-11-18
申请号：PCT/GB1999/001251
申请日：1999-05-11
IPC分类号： C07B61/00
CPC分类号： C07C45/511 , C07B61/00 , C07B2200/11 , C07C1/34 , C07C45/28 , C07C209/28 , C07C213/02 , C07C213/08 , C07C2601/08 , C07D207/16 , C07D211/62 , C07D213/30 , C07D213/89 , C07D231/06 , C07D303/04 , C07D307/44 , C07D409/12 , C40B40/04 , C40B50/14 , C40B99/00 , C07C15/44 , C07C15/52 , C07C15/50 , C07C47/55 , C07C47/54 , C07C47/575 , C07C47/542 , C07C49/255 , C07C49/217 , C07C49/753 , C07C49/235 , C07C49/683 , C07C211/52 , C07C217/58 , C07C217/84
摘要： There is described a process for the preparation of a compound which process includes a first reaction and a second reaction, wherein the process uses a first solid supported reagent in said first reaction and a second solid supported reagent in said second reaction. The process may be used to effect multi-step organic synthesis for potential applications in combinatorial chemistry and/or the preparation of chemical libraries.
摘要翻译：描述了一种制备化合物的方法，该方法包括第一反应和第二反应，其中所述方法在所述第一反应中使用第一固体支持的试剂，在所述第二反应中使用第二固体负载的试剂。该方法可用于在组合化学和/或化学文库的制备中用于潜在应用的多步有机合成。

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