公开(公告)号：WO2015053962A1

公开(公告)日：2015-04-16

申请号：PCT/US2014/057679

申请日：2014-09-26

Applicant: UOP LLC ,  BORESKOV INSTITUTE OF CATALYSIS

Inventor： BUCHBINDER, Avram M. ,  SHIH, Raymond ,  BHATTACHARYYA, Alakananda ,  JORGENSON, Evan B. ,  JARUSIRIPIPAT, Tatsamai T. ,  KUZNETSOVA, Nina

IPC: C07C51/265 ,  C07C51/43 ,  C07C63/15 ,  C07C63/26 ,  C07C63/24

CPC classification number: C07C51/29 ,  C07C51/265 ,  C07C51/43 ,  C07C63/26

Abstract: Processes have been developed to obtain recycle ionic liquid streams which are active for oxidation of alkyl aromatic compounds, and which reduce the amount of 4-CBA in the solid oxidation products. The process can reduce the makeup amount of ionic liquid, carboxylic acid, catalyst, bromine source, and ammonia source. Volatile components, including carboxylic acid, such as acetic acid, and water, and solid components, such as aromatic carboxylic acids and other crystallized products, are removed, and the proper proportion of fresh or recycled carboxylic acid, water, and ammonia source or other base are added.

Abstract translation: 已经开发了用于获得对烷基芳族化合物氧化有活性的再循环离子液体流并且减少固体氧化产物中的4-CBA的量的方法。 该方法可以减少离子液体，羧酸，催化剂，溴源和氨源的补充量。 去除挥发性成分，包括羧酸，如乙酸和水，以及固体组分，如芳族羧酸和其他结晶产物，适量比例的新鲜或再循环的羧酸，水和氨源或其他 基地被添加。

公开(公告)号：WO2012147098A3

公开(公告)日：2013-03-21

申请号：PCT/IN2012000266

申请日：2012-04-13

Applicant: GLENMARK GENERICS LTD ,  GAVHANE SACHIN BABAN ,  WAKADE SANJAY MARUTI ,  KADAM SURESH MAHADEV

Inventor： GAVHANE SACHIN BABAN ,  WAKADE SANJAY MARUTI ,  KADAM SURESH MAHADEV

IPC: C07D213/75 ,  C07C205/43

CPC classification number: C07C201/12 ,  C07B2200/13 ,  C07C45/71 ,  C07C51/29 ,  C07C205/43 ,  C07C2601/02 ,  C07D213/75 ,  C07C47/575 ,  C07C65/26

Abstract: Disclosed is a process of preparing roflumilast.

Abstract translation: 公开了一种制备罗氟司特的方法。

公开(公告)号：WO2008084472A3

公开(公告)日：2009-11-26

申请号：PCT/IL2008000013

申请日：2008-01-02

Applicant: VASCULAR BIOGENICS LTD ,  HALPERIN GIDEON ,  KOVALEVSKI-ISHAI ETI

Inventor： HALPERIN GIDEON ,  KOVALEVSKI-ISHAI ETI

IPC: C07F9/02

CPC classification number: C07B41/00 ,  C07C29/48 ,  C07C41/26 ,  C07C45/27 ,  C07C45/29 ,  C07C51/16 ,  C07C51/29 ,  C07C67/08 ,  C07C67/28 ,  C07C67/39 ,  C07F9/091 ,  C07F9/10 ,  C07F9/106 ,  Y02P20/55

Abstract: Novel synthetic routes, which are highly applicable for industrial preparation of therapeutically beneficial oxidized phospholipids are disclosed. Particularly, novel methods for efficiently preparing compounds having a glycerolic backbone and one or more oxidized moieties attached to the glycerolic backbone, which are devoid of column chromatography are disclosed. Further disclosed are novel methods of introducing phosphorous-containing moieties such as phosphate moieties to compounds having glycerolic backbone and intermediates formed thereby.

Abstract translation: 公开了高度适用于治疗有益的氧化磷脂的工业制备的新型合成路线。 特别地，公开了用于有效制备具有连接到甘油主链上的甘油主链和一个或多个氧化部分的化合物的新方法，其没有进行柱层析。 进一步公开的是将含有磷的部分例如磷酸酯部分引入具有甘油主链的化合物和由其形成的中间体的新方法。

公开(公告)号：WO2008084472A2

公开(公告)日：2008-07-17

申请号：PCT/IL2008/000013

申请日：2008-01-02

Applicant: VASCULAR BIOGENICS LTD. ,  HALPERIN, Gideon ,  KOVALEVSKI-ISHAI, Eti

Inventor： HALPERIN, Gideon ,  KOVALEVSKI-ISHAI, Eti

IPC: C07F9/02

CPC classification number: C07B41/00 ,  C07C29/48 ,  C07C41/26 ,  C07C45/27 ,  C07C45/29 ,  C07C51/16 ,  C07C51/29 ,  C07C67/08 ,  C07C67/28 ,  C07C67/39 ,  C07F9/091 ,  C07F9/10 ,  C07F9/106 ,  Y02P20/55

Abstract: Novel synthetic routes, which are highly applicable for industrial preparation of therapeutically beneficial oxidized phospholipids are disclosed. Particularly, novel methods for efficiently preparing compounds having a glycerolic backbone and one or more oxidized moieties attached to the glycerolic backbone, which are devoid of column chromatography are disclosed. Further disclosed are novel methods of introducing phosphorous-containing moieties such as phosphate moieties to compounds having glycerolic backbone and intermediates formed thereby.

Abstract translation: 公开了高度适用于治疗有益的氧化磷脂的工业制备的新型合成路线。 特别地，公开了用于有效制备具有连接到甘油主链上的甘油主链和一个或多个氧化部分的化合物的新方法，其没有进行柱层析。 进一步公开的是将含有磷的部分例如磷酸酯部分引入具有甘油主链的化合物和由其形成的中间体的新方法。

公开(公告)号：WO2014181362A1

公开(公告)日：2014-11-13

申请号：PCT/IN2014/000322

申请日：2014-05-09

Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH

Inventor： MURUGAN, Muthukrishnan ,  MOHAMMAD, Mujahid

IPC: C07C67/08 ,  C07C67/14 ,  C07C69/734 ,  C07C41/02 ,  C07C41/16 ,  C07C41/26 ,  C07C43/215 ,  C07C43/23 ,  C07C51/29 ,  C07C51/367 ,  C07C59/64

CPC classification number: C07C67/08 ,  C07C41/02 ,  C07C41/09 ,  C07C41/16 ,  C07C41/26 ,  C07C41/30 ,  C07C51/29 ,  C07C51/367 ,  C07C67/14 ,  C07C43/215 ,  C07C43/23 ,  C07C59/64 ,  C07C69/734

Abstract: The present disclosure provides a process for synthesis of 3-aryl-2-hydroxy propanoic acid derivatives of formula ( S )-1. wherein R 1 represents H or (C 1 -C 5 ) alkyl groups and R 2 represents (C 1 -C 5 ) alkyl groups.

Abstract translation: 本公开提供了合成式（S）-1的3-芳基-2-羟基丙酸衍生物的方法。 其中R1表示H或（C1-C5）烷基，R2表示（C1-C5）烷基。

公开(公告)号：WO2009147068A1

公开(公告)日：2009-12-10

申请号：PCT/EP2009/056560

申请日：2009-05-28

Applicant: F. HOFFMANN-LA ROCHE AG ,  BACHMANN, Stephan ,  HILDBRAND, Stefan ,  JAPPY, James ,  PATEL, Dinesh Maganbhai ,  PFLEGER, Christophe ,  TIDSWELL, Robert John Ernest ,  TRUSSARDI, Rene

Inventor： BACHMANN, Stephan ,  HILDBRAND, Stefan ,  JAPPY, James ,  PATEL, Dinesh Maganbhai ,  PFLEGER, Christophe ,  TIDSWELL, Robert John Ernest ,  TRUSSARDI, Rene

IPC: C07C45/00 ,  C07C51/15 ,  C07C51/285 ,  C07C51/29 ,  C07C63/70 ,  C07C47/55 ,  C07C45/51

CPC classification number: C07C45/518 ,  C07C45/00 ,  C07C51/15 ,  C07C51/285 ,  C07C51/29 ,  C07C47/55 ,  C07C63/70

Abstract: The present invention comprises a process for the preparation of 3-chloro-2-fluoro-5- trifluoromethyl benzoic acid of the formula or of a salt thereof. 3-Chloro-2-fluoro-5-trifluoromethyl benzoic acid or salts thereof are versatile intermediates for the preparation of active pharmaceutical or agrochemical agents.

Abstract translation: 本发明包括制备下式的3-氯-2-氟-5-三氟甲基苯甲酸或其盐的方法。 3-氯-2-氟-5-三氟甲基苯甲酸或其盐是用于制备活性药物或农药的多功能中间体。

公开(公告)号：WO2004067484A3

公开(公告)日：2004-11-18

申请号：PCT/US2004002475

申请日：2004-01-29

Applicant: NUTRASWEET CO

Inventor： TANIELYAN SETRAK K ,  AUGUSTINE ROBERT L ,  PRAKASH INDRA ,  FURLONG KENNETH E ,  SCHERM ROBERT C ,  JACKSON HANDLEY E

IPC: C07C20060101 ,  C07C45/29 ,  C07C45/30 ,  C07C51/29

CPC classification number: C07C45/30 ,  C07C45/29 ,  C07C45/294 ,  C07C51/29 ,  C07C53/126

Abstract: The present invention relates to a process of oxidation of alcohols selectively to aldehydes or ketones with NaOCI using a TEMPO - borate catalyst system. It is shown that the oxidation can be efficiently carried out without KBr additives under solvent free conditions. Aldehydes such as 3,3-dimethylbutyraldehyde can be produced efficiently using the present invention.

Abstract translation: 本发明涉及使用TEMPO-硼酸盐催化剂体系将醇用NaOCl选择性地氧化成醛或酮的方法。 结果表明，在无溶剂条件下，不用KBr添加剂就可以有效地进行氧化。 使用本发明可以有效地制造3,3-二甲基丁醛等醛类。

公开(公告)号：WO2002090306A1

公开(公告)日：2002-11-14

申请号：PCT/IB2002/001402

申请日：2002-04-18

Applicant: WARNER-LAMBERT COMPANY ,  BLAKEMORE, David, Clive ,  BRYANS, Justin, Stephen

Inventor： BLAKEMORE, David, Clive ,  BRYANS, Justin, Stephen

IPC: C07C49/433

CPC classification number: C07C303/28 ,  C07B2200/07 ,  C07C17/093 ,  C07C29/147 ,  C07C45/676 ,  C07C49/433 ,  C07C51/29 ,  C07C2601/04 ,  C07C2601/16 ,  C07C2602/20 ,  C07C2602/22 ,  C07C22/02 ,  C07C55/28 ,  C07C309/66 ,  C07C33/14

Abstract: This invention relates to a process for the production of the cyclic ketone (1R,5S)-bicyclo[3.2.0]heptan-3-one. This compound is useful inter alia as an intermediate for the synthesis of analogues of gabapentin (Neurontin®). The reaction process is illustrated by the following scheme.

Abstract translation: 本发明涉及一种制备环酮（1R，5S） - 双环[3.2.0]庚-3-酮的方法。 该化合物尤其可用作合成加巴喷丁类似物（Neurontin？）的中间体。 反应过程由以下方案说明。

公开(公告)号：WO98049130A2

公开(公告)日：1998-11-05

申请号：PCT/US1998/008544

申请日：1998-04-28

IPC: C07C51/29 ,  C07C51/377 ,  C07C65/11 ,  C07C67/343 ,  C07C235/66 ,  C07C69/76 ,  C07C63/34 ,  C07C233/00

CPC classification number: C07C235/66 ,  C07C51/29 ,  C07C51/377 ,  C07C65/11 ,  C07C67/343 ,  C07C65/24 ,  C07C63/36 ,  C07C69/734

Abstract: In one embodiment, the present invention provides a compound comprising formula (I), wherein A = H or OH, X = OH, a halogen, OR, NHR, NR', R'' where R, R', and R'' = H, C1-8alkyl, C2-8alkenyl, or C2-8alkynyl, cycloalkyl, cycloalkenyl, aryl, aralkyl or heterocyclic, substituted or unsubstituted; and R1,R2,R3,R4,R5 = H, C1-8alkyl, C2-8alkenyl, or C2-8alkynyl, cycloalkyl, cycloalkenyl, aryl or heterocyclic, substituted or unsubstituted, wherein R1 includes at least one methylene spacer through which R1 is attached to said compound. The present invention also provides methods for making hydroxynaphthoic acids.

Abstract translation: 在一个实施方案中，本发明提供包含式（I）的化合物，其中A = H或OH，X = OH，卤素，OR，NHR，NR'，R“，其中R，R'和R” = H，C 1-8烷基，C 2-8烯基或C 2-8炔基，环烷基，环烯基，芳基，芳烷基或杂环，取代或未取代的; R 1，R 2，R 3，R 4，R 5 = H，C 1-8烷基，C 2-8烯基或C 2-8炔基，环烷基，环烯基，芳基或杂环，取代或未取代的，其中R 1包括至少一个亚甲基间隔基， 附着于所述化合物。 本发明还提供了制备羟基萘甲酸的方法。

公开(公告)号：WO2013080896A1

公开(公告)日：2013-06-06

申请号：PCT/JP2012/080401

申请日：2012-11-16

Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED

Inventor： ISHIKAWA, Junichi

IPC: C07C29/36 ,  C07C33/20 ,  C07C51/27 ,  C07C51/29 ,  C07C57/30

CPC classification number: C07C51/29 ,  C07C29/36 ,  C07C33/20 ,  C07C51/27 ,  C07C57/30

Abstract: A method for producing 2,6-diethyl-4-methylphenylacetic acid comprising a step of reacting a 2,6-diethyl-4-methylphenyl magnesium halide with ethylene oxide to obtain 2-(2,6-diethyl-4-methylphenyl) ethanol; and a step of oxidizing 2-(2,6-diethyl-4-methylphenyl) ethanol. The oxidation is conducted preferably further in the presence of a nitroxyl radical, and more preferably in the presence of a salt of a hypohalous acid and/or a salt of a halous acid.

Abstract translation: 一种2,6-二乙基-4-甲基苯乙酸的制造方法，其特征在于，使2,6-二乙基-4-甲基苯基卤化镁与环氧乙烷反应，得到2-（2,6-二乙基-4-甲基苯基）乙醇 ; 和氧化2-（2,6-二乙基-4-甲基苯基）乙醇的步骤。 优选在硝酰基存在下进一步进行氧化，更优选在次卤酸和/或盐酸盐的存在下进行氧化。