公开(公告)号：EP2417119A2

公开(公告)日：2012-02-15

申请号：EP10761972.8

申请日：2010-04-01

Applicant: The Regents of The University of California

Inventor： SATYAMURTHY, Nagichettiar ,  BARRIO, Jorge, R.

IPC: C07D319/06 ,  C07D263/04 ,  C07D239/10

CPC classification number: C07D319/06 ,  C07B59/00 ,  C07B2200/05 ,  C07C201/12 ,  C07C227/16 ,  C07C229/36 ,  C07D233/32 ,  C07D241/08 ,  C07D263/18 ,  C07D405/12 ,  C07D413/12 ,  C07C205/11

Abstract: Phenyliodonium ylide derivatives substituted with electron donating as well as electron withdrawing groups on the aromatic ring are shown for use as precursors in aromatic nucleophilic substitution reactions. The iodonium ylide group is substituted by nucleophiles such as halide ions to provide the corresponding haloaryl derivatives. No- carrier-added [F-18]fluoride ion exclusively substitutes the iodonium ylide moiety in these derivatives and provides high specific activity F- 18 labeled fluoro derivatives. Protected L-dopa-6-iodonium ylide derivative have been synthesized as a precursors for the preparation of no-carrier-added 6-[F- 18]fluoro-L-dopa. The iodonium ylide group in this L-dopa.derivative is nucleophilically substituted by no-carrier-added [F-18]fluoride ion to provide a [F-18]fluoro intermediates which upon acid hydrolysis yielded 6-[F- 18]fluoro-L-dopa.

公开(公告)号：EP1831144B1

公开(公告)日：2011-08-17

申请号：EP05816593.7

申请日：2005-12-07

Applicant: Richter Gedeon Nyrt.

Inventor： VASS, András ,  DUDÁS, József ,  BORBÉLY, László ,  HAÁSZ, Ferenc ,  JEKKEL, Péter

IPC: C07C37/50 ,  C07C39/17 ,  C07C39/26

CPC classification number: C07C37/055 ,  C07C45/673 ,  C07C49/755 ,  C07C49/84 ,  C07C51/367 ,  C07C201/12 ,  C07C2602/10 ,  C07J1/0059 ,  C07J1/0074 ,  C07C65/03 ,  C07C65/10 ,  C07C39/04 ,  C07C39/14 ,  C07C39/07 ,  C07C39/28 ,  C07C39/27 ,  C07C39/08 ,  C07C39/17 ,  C07C205/22

Abstract: The invention relates to a process for the preparation of a phenolic hydroxy-substituted compound of the general formula (I) by desalkylation of an alkyl aryl ether of the general formula (II) by treatment with a thiourea/aluminium chloride reagent pair, in said general formulae R1 stands for straight chain or branched C1-6 alkyl group; R2, R3, R4, R5 , and R6 have the same or different meanings and stand for hydrogen or halogen atom, hydroxy, carboxy, nitro, oxo, C1-6 alkylcarbonyl, straight chain or branched alkyl or - alkoxy, or aryl group, or R2 and R3 together stand for a 5-7 membered ring or fused ring system; said 5-7 membered ring may be a partially saturated ring optionally substituted with an oxo group or can be an unsaturated ring; or said fused ring system may constitute with the first ring a steroid, preferably an estratriene derivative optionally substituted with an oxo or C1-6 alkylcarbonyloxy group in the 17 position -.

Abstract translation: 本发明涉及一种制备通式（I）的酚类羟基取代的化合物的方法，该方法通过在所述的硫脲/氯化铝试剂对中用硫脲/氯化铝试剂对进行脱烷基处理而得到通式（Ⅱ）的烷基芳基醚 通式R1代表直链或支链C 1-6烷基; R2，R3，R4，R5和R6具有相同或不同的含义，代表氢或卤原子，羟基，羧基，硝基，氧代，C1-6烷基羰基，直链或支链烷基或 - 烷氧基或芳基， 或R 2和R 3一起代表5-7元环或稠环体系; 所述5-7元环可以是任选被氧代基取代的部分饱和的环，或者可以是不饱和环; 或所述稠环体系可以与第一环一起构成类固醇，优选在17位上任选被氧代或C 1-6烷基羰基氧基取代的雌三烯衍生物。

公开(公告)号：EP1369412B1

公开(公告)日：2011-07-27

申请号：EP03011471.4

申请日：2003-05-21

Applicant: Bayer MaterialScience AG

Inventor： Zechlin, Joachim, Dr. ,  Verkerk, Kai, Dr. ,  Wastian, Dietmar ,  Joschek, Katrin, Dr. ,  Loddenkemper, Tim ,  Pinke, Wilfried ,  Schelhaas, Michael, Dr. ,  Ronge, Georg, Dr.

IPC: C07C205/45 ,  C07C205/56 ,  C07C211/60 ,  C07C209/22 ,  C07C209/36 ,  C07C263/10

CPC classification number: C07C209/68 ,  C07C201/12 ,  C07C211/58 ,  C07C263/10 ,  C07C265/14 ,  C07C205/56 ,  C07C205/45

公开(公告)号：EP2311792A1

公开(公告)日：2011-04-20

申请号：EP09012899.2

申请日：2009-10-13

Applicant: Roche Diagnostics GmbH ,  F.Hoffmann-La Roche AG

Inventor： Knipp, Bernhard

IPC: C07C201/12 ,  C07C205/45

CPC classification number: C07C201/12 ,  C07C205/45 ,  C07D317/18 ,  C07D319/06

Abstract: Die vorliegende Erfindung betrifft ein Syntheseverfahren enthaltend die folgenden Schritte (i) Umsetzung von 3-Ethyl-4-nitrobenzoesäure mit Thionylchlorid zur Erzeugung eines 3-Ethyl-4-nitrobenzoesäurechlorids oder mittels Wasserabspaltung aus 3-Ethyl-4-nitrobenzoesäure eines 3-Ethyl-4-nitrobenzoesäureanhydrids und (ii) Friedel-Crafts-Acylierung durch Reaktion des 3-Ethyl-4-nitrobenzoesäurechlorids oder des 3-Ethyl-4-nitrobenzoesäureanhydrids mit gegebenenfalls substituiertem Aryl-H, so dass gegebenenfalls substituiertes (3-Ethyl-4-nitrophenyl)-aryl-methanon entsteht. Darüber hinaus betrifft die vorliegende Erfindung Verbindungen enthaltend (3-Ethyl-4-nitrophenyl)-aryl-methanon, dadurch gekennzeichnet, dass das gegebenenfalls substituierte Aryl ein gegebenenfalls substituierter kondensierter Aromat ist.

Abstract translation: 合成方法包括：（a）使3-乙基-4-硝基苯甲酸与亚硫酰卤反应生成3-乙基-4-硝基苯甲酰卤; 和（b）通过使3-乙基-4-硝基苯甲酰氯或3-乙基-4-硝基苯甲酸酐与任选取代的芳基-H反应形成任选取代的（3-乙基-4-硝基苯甲酸） 硝基 - 苯基） - 芳基 - 甲酮。 包括独立权利要求：（1）（3-乙基-4-硝基苯基） - 芳基 - 甲酮或[3-（2-羟基-1-甲基 - 乙基）-4-硝基苯基] - 芳基 - 甲酮，其中 芳基是稠合的芳族化合物，其任选被取代; 和（2）在5'或3'位置含有取代基的核苷，其中取代基是[3-（2-O-1-甲基 - 乙基）-4-硝基苯基] - 芳基 - 甲酮。

公开(公告)号：EP2027105A4

公开(公告)日：2011-04-13

申请号：EP07748103

申请日：2007-05-07

Applicant: ASTRAZENECA AB

Inventor： AINGE DEBRA ,  CORNWALL PHILIP ,  GILL DUNCAN MICHAEL ,  KUMAR VINOD ,  O'KEEFE PHILIP ,  SINCLAIR RHONA ,  VAZ LUIS-MANUEL ,  WAY EDWARD LAURENCE

IPC: C07D317/10 ,  A61K31/40 ,  A61P29/00 ,  C07C205/06 ,  C07C209/66 ,  C07C211/46 ,  C07C211/48 ,  C07D303/22

CPC classification number: C07D317/22 ,  C07C201/08 ,  C07C201/12 ,  C07C205/26 ,  C07C205/37 ,  C07C233/25 ,  C07D211/58 ,  C07D303/22

公开(公告)号：EP2174927A4

公开(公告)日：2011-01-26

申请号：EP08791756

申请日：2008-07-28

Applicant: SUMITOMO CHEMICAL CO

Inventor： TAKEDA MASAHIRO ,  KADONO HIROSHI ,  MURAKAMI KAZUO

IPC: C07C201/12 ,  C07C205/09

CPC classification number: C07C201/12 ,  C07C205/09

公开(公告)号：EP2011764A4

公开(公告)日：2010-08-18

申请号：EP07742874

申请日：2007-04-26

Applicant: SUMITOMO CHEMICAL CO

Inventor： HAGIYA KOJI ,  SASAKI KAZUAKI

IPC: C01D3/02 ,  C07B39/00 ,  C07C17/20 ,  C07C22/08 ,  C07C67/307 ,  C07C69/76 ,  C07C201/12 ,  C07C205/11

CPC classification number: C07B39/00 ,  C01D3/02 ,  C07C17/208 ,  C07C67/14 ,  C07C201/12 ,  C07C22/08 ,  C07C69/76 ,  C07C205/12

公开(公告)号：EP2196468A1

公开(公告)日：2010-06-16

申请号：EP10001846.4

申请日：2006-01-12

Applicant: Schering Corporation

Inventor： Wu, George G. ,  Sudhakar, Anantha ,  Wang, Tao ,  Xie, Ji ,  Chen, Frank Xing ,  Poirier, Marc ,  Huang, Mingsheng ,  Sabesen, Vijay ,  Kwok, Daw-long ,  Cui, Jian ,  Yang, Xiaojing ,  Thiruvengadam, Tiruvettipuram K. ,  Liao, Jing

IPC: C07F9/58

CPC classification number: C07D263/56 ,  C07C69/606 ,  C07C69/732 ,  C07C201/10 ,  C07C201/12 ,  C07C205/44 ,  C07C205/55 ,  C07C231/10 ,  C07C231/12 ,  C07C235/28 ,  C07C303/32 ,  C07C309/08 ,  C07C2601/16 ,  C07D277/64 ,  C07D307/92 ,  C07D333/56 ,  C07D405/06 ,  C07D413/06 ,  C07D417/06 ,  C07F7/1852 ,  C07F9/582 ,  Y02P20/55 ,  C07C233/28

Abstract: This application discloses a compound which is useful in the preparation of himbacine analogs as well as processes for its preparation:

wherein R 9 is selected from the group consisting of C 1 -C 10 alkyl, aryl, heteroaryl, and arylalkyl.

Abstract translation: 本申请公开了一种可用于制备烟肼类似物的化合物及其制备方法：其中R 9选自C 1 -C 10烷基，芳基，杂芳基和芳基烷基。

公开(公告)号：EP1568681B1

公开(公告)日：2010-04-28

申请号：EP03812296.6

申请日：2003-11-21

Applicant: Mitsui Chemicals, Inc.

Inventor： KUMAMOTO, Yukihiro c/o Mitsui Chemicals, Inc. ,  TAKAOKA, Masazumi c/o Mitsui Chemicals, Inc. ,  MIZUTA, Hideki c/o Mitsui Chemicals, Inc. ,  MATSUZAKI, Yoriaki c/o Mitsui Chemicals, Inc.

IPC: C07C209/18 ,  C07C209/36 ,  C07C211/57

CPC classification number: C07C209/18 ,  C07C201/12 ,  C07C211/58 ,  C07C205/25

Abstract: A process for producing 1,5-diaminonaphthalene which comprises dehydrogenating a 5-substituted 1-tetralone to produce a naphthol compound and then aminating the hydroxy group of the naphthol compound. Thus, the target compound can be produced without yielding the 1,8-diamino isomer as a by-product and without via a nitroimine or nitroenamine, which is unstable, as an intermediate.

公开(公告)号：EP2176244A2

公开(公告)日：2010-04-21

申请号：EP08797091.9

申请日：2008-08-04

Applicant: E. I. du Pont de Nemours and Company

Inventor： ANNIS, Gary, David ,  SMITH, Brenton, Todd

IPC: C07D261/04 ,  C07D413/10 ,  C07D413/12 ,  C07D417/12 ,  C07C49/235

CPC classification number: C07D261/04 ,  C07C45/65 ,  C07C45/68 ,  C07C45/72 ,  C07C49/813 ,  C07C49/83 ,  C07C49/835 ,  C07C49/84 ,  C07C65/38 ,  C07C69/007 ,  C07C201/12 ,  C07C205/45 ,  C07D413/10 ,  C07D413/12 ,  C07D417/12

Abstract: Disclosed is a method for preparing a compound of Formula: (1); wherein R1 is CHX2, CX3, CX2CHX2 or CX2CX3; each X is independently Cl or F; Z is optionally substituted phenyl; and Q is phenyl or 1-naphthalenyl, each optionally substituted as defined in the disclosure; comprising contacting a compound of Formula: (2).