公开(公告)号：EP2170804A1

公开(公告)日：2010-04-07

申请号：EP08760854.3

申请日：2008-06-11

Applicant: Saltigo GmbH

Inventor： MÜLLER, Thomas-Norbert ,  DOCKNER, Michael

IPC: C07C205/37 ,  C07C201/12

CPC classification number: C07C205/37 ,  C07B41/04 ,  C07C45/515 ,  C07C201/12

Abstract: A method of producing 2-phenoxyacetals of the general formula (Ia) is likewise described in which R1 is hydrogen, a branched or unbranched C1-C12-alkyl moiety, a low-electron, halogen-NO2-, -CN, -CF3-, acyl- or branched or unbranched alkyl-substituted or unsubstituted C5-C6-aryl or heteroaryl moiety and R2 is a branched or unbranched C1-C5-alkyl moiety or both R2 moieties are directly linked to one another or via a C1-C4 unit, one Y is always hydrogen and the other Y is an -NO2, -CN or -CF3 moiety or fluorine or chlorine or both Y moieties each independently of one another are an NO2-, CN- or CF3-moiety or fluorine or chlorine, Z is hydrogen or an -NO2 moiety or branched or unbranched C1-C6-alkyl moiety or acyl moiety, by reacting a 2-hydroxyacetal compound of the general formula (II) in which R1 and R2 have the meaning given for formula (Ia) with a substituted aromatic of the general formula (III) in which Y has the meaning given for formula (I) and Y is fluorine, chlorine, bromine or an NO2 group, in the presence of a base. A method of producing the corresponding 2-phenoxycarbaldehydes by acid hydrolysis of the 2-phenoxyacetals is likewise described.

公开(公告)号：EP1700841A3

公开(公告)日：2010-02-24

申请号：EP06013050.7

申请日：2001-07-26

Applicant: Shire US Inc.

Inventor： Lang, Philip Charles ,  Spencer, Roxanne Paula ,  Yeh, Wen-Lung ,  Roth, Michael Joseph

IPC: C07C201/08 ,  C07C201/12 ,  C07C201/14 ,  C07D487/04 ,  C07C209/36

CPC classification number: C07D487/04 ,  C07C201/08 ,  C07C201/12 ,  C07C227/04 ,  C07C227/16 ,  C07C229/16 ,  C07C205/12 ,  C07C205/26 ,  C07C205/44

Abstract: Methods are provided for making certain 6,7-dihalo-1,5-dihydroimidazo [2,1-b] quinazolin-2 (3H) -ones from 2,3-dihalobenzaldehydes. A method is also provided for making the intermediate ethyl N-(2,3-dihalo-6-nitrobenzyl)glycines from 2,3-dihalobenzaldehydes and for reducing the glycine compounds using either SnCl 2 or a specially defined catalyst. A cyclization method to form the desired 6,7-dihalo-1,5-dihydroimidazo[2,1-b]quinazolin-2(3H)-ones from the corresponding iminoquinazoline compounds is further provided. These methods are particularly suitable in the manufacture of Anagrelide base.

公开(公告)号：EP2065357A1

公开(公告)日：2009-06-03

申请号：EP08169219.6

申请日：2008-11-17

Applicant: Saltigo GmbH

Inventor： Cotté, Alain ,  Müller, Nikolaus ,  Gotta, Matthias ,  Beller, Matthias ,  Schareina, Thomas ,  Zapf, Alexander

IPC: C07C41/16 ,  C07C43/18

CPC classification number: C07C41/16 ,  C07C201/12 ,  C07C213/00 ,  C07C231/12 ,  C07D213/643 ,  C07C217/90 ,  C07C233/25 ,  C07C205/38 ,  C07C43/275 ,  C07C43/263 ,  C07C43/257

Abstract: Described is a process for preparing diaryl ethers of the formula (I)

         Ar-O-Ar'     (I)

In which Ar is an aryl or substituted aryl group and Ar' is an aryl, substituted aryl, heteroaryl or substituted heteroaryl group,
by reacting an aryl of formula (II) or a aryloxy salt of formula (III)

         Ar-OH     (II)

         Ar-OR     (III)

In which Ar has the same meaning as in formula (I) and R is an alkali metal,
with an aryl or heteroaryl bromide of formula (IV)

         Ar'-Br     (IV)

In which Ar' has the same meaning as in formula (I),
characterized in that the reaction is carried out in the presence of a copper(I)salt and a 1-substituted imidazole as catalyst system.

Abstract translation: 描述了制备式（I）的二芳基醚的方法。ƒ€ƒ€ƒ€ƒ€ƒ€ƒAr-O-Ar'€ƒ€ƒ€ƒ€ƒ（I）In 其中Ar是芳基或取代的芳基，Ar'是芳基，取代的芳基，杂芳基或取代的杂芳基，通式（II）的芳基或式（III）的芳氧基盐反应€ƒ€ƒ€ ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ（II）€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ （III）其中Ar与式（I）中的含义相同，R为碱金属，与式（Ⅳ）的芳基或杂芳基溴化合物反应，ƒ€ƒ€ƒ€ƒ€ƒ （Ⅳ）其中Ar'与式（I）中的含义相同，其特征在于反应在铜的存在下进行 （I）盐和1-取代咪唑作为催化剂体系。

公开(公告)号：EP2057174A1

公开(公告)日：2009-05-13

申请号：EP07788423.7

申请日：2007-08-14

Applicant: Evonik Degussa GmbH

Inventor： PLENIO, Herbert ,  FLECKENSTEIN, Christoph ,  KADYROV, Renat ,  ALMENA, Juan ,  MONSEES, Axel ,  RIERMEIER, Thomas

IPC: C07F9/54 ,  C07F9/50 ,  B01J27/185 ,  C07B37/02

CPC classification number: C07C2/88 ,  B01J31/2404 ,  B01J31/2447 ,  B01J2231/321 ,  B01J2231/4227 ,  B01J2231/4266 ,  B01J2231/4283 ,  B01J2531/824 ,  C07C17/26 ,  C07C41/30 ,  C07C45/62 ,  C07C201/12 ,  C07C209/68 ,  C07C253/30 ,  C07D213/16 ,  C07D213/22 ,  C07D213/73 ,  C07D265/30 ,  C07F9/5022 ,  C07F9/5442

Abstract: The invention is directed to a phosphine compound represented by general formula (1) wherein R' and R' independently are selected from alkyl, cycloalkyl and 2-furyl radicals, or R' and R' are joined together to form with the phosphorous atom a carbon-phosphorous monocycle comprising at least 3 carbon atoms or a carbon- phosphorous bicycle; the alkyl radicals, cycloalkyl radicals, and carbon-phosphorous monocycle being unsubstituted or substituted by at least one radical selected from the group of alkyl, cycloalkyl, aryl, alkoxy, and aryloxy radicals; Cps is a partially substituted or completely substituted cyclopentadien-1-yl group, including substitutions resulting in a fused ring system, and wherein a substitution at the 1- position of the cyclopentadien-1-yl group is mandatory when the cyclopentadien-1-yl group is not part of a fused ring system or is part of an indenyl group. Also claimed is the use of these phosphines as ligands in catalytic reactions and the preparation of these phosphines.

公开(公告)号：EP2055689A1

公开(公告)日：2009-05-06

申请号：EP09000403.7

申请日：2004-05-17

Applicant: Sumitomo Chemical Company, Limited ,  Carreira, Erick M.

Inventor： Carreira, Erick, M.

IPC: C07B53/00 ,  C07C201/12 ,  C07C201/14 ,  C07C205/04 ,  C07C205/09 ,  C07C205/15 ,  C07C205/16 ,  C07C205/37 ,  C07C205/45 ,  C07C209/34 ,  C07C211/28 ,  C07C231/12 ,  C07C231/18 ,  C07D213/06 ,  C07D213/38 ,  C07D307/12 ,  C07D307/38 ,  C07D307/52 ,  C07D307/58 ,  C07D309/04 ,  C07D309/06 ,  C07D333/12 ,  C07D333/20

CPC classification number: C07B53/00 ,  C07B2200/07 ,  C07C201/12 ,  C07C231/18 ,  C07D213/38 ,  C07D307/12 ,  C07D307/52 ,  C07D309/04 ,  C07D333/20 ,  C07C233/13 ,  C07C233/66 ,  C07C205/04 ,  C07C205/09 ,  C07C205/15 ,  C07C205/16 ,  C07C205/32 ,  C07C205/45

Abstract: A method for producing an optically active nitro compound having two hydrogen atoms on its α-carbon atom and having β-asymmetric carbon atom which comprises making an α, β-unsaturated nitroolefin having a hydrogen atom on its α-carbon atom react with at least one organosilicon compound having at least one silicon-hydrogen bond in the molecule in the presence of an asymmetric copper complex and water.

Abstract translation: 一种在其± - 碳原子上具有2-不对称碳原子的具有2个氢原子的光学活性硝基化合物的方法，其包括在其± - 碳原子上制备具有氢原子的±，2不饱和的硝基烯烃至少与 一种在不对称铜配合物和水的存在下在分子中具有至少一个硅氢键的有机硅化合物。

公开(公告)号：EP2054365A2

公开(公告)日：2009-05-06

申请号：EP07763806.2

申请日：2007-07-06

Applicant: Uniban - Universidade Bandeirante De São Paulo ,  Fundaçao de Amparo à Pesquisa do Estado de Sao Paulo - FAPESP

Inventor： SUÁREZ, José, Agustín, Quincoces ,  MARIA, Durvanei, Augusto ,  RANDO, Daniela, Gonçales ,  MARTINS, Clizete, Aparecida, Sbravate ,  PARDI, Paulo, Celso ,  DE SOUZA, Pamela, Oliveira

IPC: C07C45/64 ,  C07C45/69 ,  C07C45/74 ,  C07C49/223 ,  C07C49/603 ,  A61K31/121 ,  A61K31/122

CPC classification number: C07C255/37 ,  C07C45/64 ,  C07C49/255 ,  C07C51/367 ,  C07C59/90 ,  C07C67/14 ,  C07C69/78 ,  C07C201/12 ,  C07C205/37 ,  C07C205/45 ,  C07C253/30 ,  C07C2601/14 ,  C07C255/46

Abstract: The present invention refers to new derivatives of the penta-1,4-dien-3-ones, as well as their processes of preparation. These compounds present strong antitumoral activity and promising antiparasitic action, behaving as almost atoxic by laboratory assays and also by hystopathologic studies. The present invention refers also to a pharmaceutical composition consisting of the referred compounds, method of treatment for cancer and parasitic diseases.

公开(公告)号：EP2053032A1

公开(公告)日：2009-04-29

申请号：EP07805906.0

申请日：2007-08-08

Applicant: Kaneka Corporation

Inventor： AMANO, Susumu ,  FUJII, Akio ,  YAMAMOTO, Shohei ,  MITSUDA, Masaru

IPC: C07B53/00 ,  C07C51/367 ,  C07C59/48 ,  C07C201/12 ,  C07C205/56 ,  C07B61/00

CPC classification number: C07B53/00 ,  C07B2200/07 ,  C07C51/00 ,  C07C51/367 ,  C07C201/12 ,  C07C59/48 ,  C07C205/56

Abstract: The present invention has its object to provide a method for producing an optically active hydroxycarboxylic acid derivative which is an intermediate important for production of medicines, agrochemicals, chemical products, and so on. The production method of the present invention comprises: carrying out a hydrogen-transfer reduction of a ketocarboxylic acid or a salt thereof by the reaction of an optically active diamine complex to produce an optically active hydroxycarboxylic acid derivative. According to the present invention, it is possible to safely and efficiently produce an industrially-useful optically active hydroxycarboxylic acid derivative.

Abstract translation: 本发明的目的是提供一种制备光学活性羟基羧酸衍生物的方法，该方法是生产药物，农用化学品，化学产品等的重要中间体。 本发明的制造方法包括：通过光学活性二胺配合物的反应进行酮羧酸或其盐的氢转移还原，制造光学活性羟基羧酸衍生物。 根据本发明，可以安全有效地制造工业上有用的光学活性羟基羧酸衍生物。

公开(公告)号：EP1867626A3

公开(公告)日：2008-07-23

申请号：EP07116762.1

申请日：2003-02-27

Applicant: Sumitomo Chemical Company, Limited ,  ONO PHARMACEUTICAL CO., LTD.

Inventor： Hibino, Hiroaki ,  Ohtsuka, Susumu ,  Miyamoto, Yasunobu ,  Yoshida, Tomoyasu ,  Okumoto, Itsuo

IPC: C07C201/12 ,  C07C205/37 ,  C07C67/307 ,  C07C69/63 ,  C07D311/24

CPC classification number: C07C205/37 ,  C07C201/12 ,  C07D311/24

Abstract: A process for producing a dicarboxylic acid compound represented by the formula (4):

wherein R 1 and R 2 are the same or different and each represents lower alkyl and the wavy line indicates that this compound is the E- or Z-isomer or a mixture of them, characterized by reacting a compound represented by the formula (2):

wherein R 1 , R 2 and the wavy line have the same meanings as the above, and one of X 2 and X 3 represents hydrogen and the other represents halogen, with nitrophenol represented by the formula (3):

in the presence of a base; a process for producing a nitrochromone compound represented by the formula (5):

wherein R 1 has the same meaning as the above, characterized by reacting the dicarboxylic acid compound or carboxylic acid thereof with an acid; a process for producing an aminochromone compound which comprises reducing the nitrochromone compound; and a process for producing an amidochromone compound which comprises acylating the aminochromone compound are provided.

公开(公告)号：EP1827678A4

公开(公告)日：2008-04-09

申请号：EP05778890

申请日：2005-08-31

Applicant: TOTAL SYNTHESIS LTD

Inventor： ORGAN MICHAEL ,  COMER EAMON

IPC: B01J19/12 ,  B01J19/00

CPC classification number: B01J19/0046 ,  B01J19/0093 ,  B01J19/126 ,  B01J23/44 ,  B01J31/0237 ,  B01J31/0239 ,  B01J31/04 ,  B01J31/2239 ,  B01J31/2265 ,  B01J31/2404 ,  B01J37/0215 ,  B01J37/031 ,  B01J2219/00286 ,  B01J2219/00333 ,  B01J2219/00344 ,  B01J2219/00367 ,  B01J2219/00369 ,  B01J2219/00389 ,  B01J2219/00418 ,  B01J2219/00423 ,  B01J2219/00585 ,  B01J2219/0059 ,  B01J2219/00599 ,  B01J2219/0072 ,  B01J2219/00747 ,  B01J2219/00788 ,  B01J2219/00822 ,  B01J2219/00824 ,  B01J2219/00831 ,  B01J2219/00835 ,  B01J2219/0086 ,  B01J2219/00862 ,  B01J2219/00873 ,  B01J2219/00891 ,  B01J2219/00941 ,  B01J2219/1227 ,  B01J2231/4211 ,  B01J2231/4261 ,  B01J2231/543 ,  B01J2531/821 ,  B01J2531/824 ,  B01J2531/96 ,  C07C1/321 ,  C07C41/30 ,  C07C45/65 ,  C07C45/68 ,  C07C51/353 ,  C07C67/343 ,  C07C201/12 ,  C07C209/02 ,  C07C213/08 ,  C07C253/30 ,  H05B6/806 ,  C07C15/14 ,  C07C47/54 ,  C07C49/794 ,  C07C49/86 ,  C07C47/546 ,  C07C47/575 ,  C07C63/04 ,  C07C69/618 ,  C07C69/65 ,  C07C69/734 ,  C07C211/52 ,  C07C217/58 ,  C07C217/60 ,  C07C255/34 ,  C07C205/06 ,  C07C205/56 ,  C07C43/215 ,  C07C43/23 ,  C07C43/205

Abstract: A reactor apparatus includes at least one reaction capillary having a lumen for receiving a reactant to undergo a reaction, and a magnetron for irradiating reactant contained in at least a portion of the capillary with microwaves. A method of micro-reacting a reactant includes providing a capillary, and irradiating the reactant in the capillary with microwaves to facilitate a chemical reaction in the capillary by which the reactant is converted into a desired product.

公开(公告)号：EP1894938A1

公开(公告)日：2008-03-05

申请号：EP06119870.1

申请日：2006-08-31

Applicant: Evonik Degussa GmbH

Inventor： Plenio, Herbert ,  Fleckenstein, Christoph ,  Kadyrov, Renat ,  Almena, Juan ,  Monsees, Axel ,  Riermeier, Thomas

IPC: C07F9/54 ,  C07F9/50 ,  B01J27/185 ,  C07B37/02

CPC classification number: C07C2/88 ,  B01J31/2404 ,  B01J31/2447 ,  B01J2231/321 ,  B01J2231/4227 ,  B01J2231/4266 ,  B01J2231/4283 ,  B01J2531/824 ,  C07C17/26 ,  C07C41/30 ,  C07C45/62 ,  C07C201/12 ,  C07C209/68 ,  C07C253/30 ,  C07D213/16 ,  C07D213/22 ,  C07D213/73 ,  C07D265/30 ,  C07F9/5022 ,  C07F9/5442

Abstract: The invention is directed to a phosphine compound represented by general formula (1)

wherein
R' and R" independently are selected from alkyl, cycloalkyl and 2-furyl radicals, or R' and R" are joined together to form with the phosphorous atom a carbon-phosphorous monocycle comprising at least 3 carbon atoms or a carbon-phosphorous bicycle; the alkyl radicals, cycloalkyl radicals, and carbon-phosphorous monocycle being unsubstituted or substituted by at least one radical selected from the group of alkyl, cycloalkyl, aryl, alkoxy, and aryloxy radicals;
Cp s is a partially substituted or completely substituted cyclopentadien-1-yl group, including substitutions resulting in a fused ring system, and wherein a substitution at the 1-position of the cyclopentadien-1-yl group is mandatory when the cyclopentadien-1-yl group is not part of a fused ring system or is part of an indenyl group. Also claimed is the use of these phosphines as ligands in catalytic reactions and the preparation of these phosphines.

Abstract translation: 本发明涉及由通式（1）表示的膦化合物，其中R'和R“独立地选自烷基，环烷基和2-呋喃基，或者R'和R”连接在一起形成磷原子a 包含至少3个碳原子的碳 - 磷单环或碳 - 磷自行车; 烷基，环烷基和碳 - 磷单环未被取代或被至少一个选自烷基，环烷基，芳基，烷氧基和芳氧基的基团取代; Cp是部分取代的或完全取代的环戊二烯-1-基，包括导致稠环体系的取代，并且其中当环戊二烯-1-基的1-位上的取代是必需的， 基团不是稠合环系统的一部分或者是茚基基团的一部分。 还要求的是在催化反应中使用这些膦作为配体并制备这些膦。