公开(公告)号：US08304550B2

公开(公告)日：2012-11-06

申请号：US12275316

申请日：2008-11-21

Applicant: Alain Cotte ,  Nikolaus Muller ,  Matthias Gotta ,  Matthias Beller ,  Thomas Schareina ,  Alexander Zapf

Inventor： Alain Cotte ,  Nikolaus Muller ,  Matthias Gotta ,  Matthias Beller ,  Thomas Schareina ,  Alexander Zapf

IPC: C07D213/63 ,  C07C209/00 ,  C07C41/01 ,  B01J31/18

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）Ar-O-Ar'（I）的二芳基醚的方法，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，由 使式（II）的芳基或式（III）的芳氧基盐Ar-OH（II）Ar-OR（III）反应其中Ar具有与式（I）中相同的含义，R是碱金属，与 式（Ⅳ）的芳基或杂芳基溴Ar'-Br（Ⅳ）其中Ar'具有与式（I）中相同的含义，其特征在于该反应在铜（I）盐 和1-取代的咪唑作为催化剂体系。

公开(公告)号：US20120202934A1

公开(公告)日：2012-08-09

申请号：US13500449

申请日：2010-10-08

Applicant: Ian Anthony Tomlinson ,  Glenn Nelson Robinson ,  Asghar Akber Peera

Inventor： Ian Anthony Tomlinson ,  Glenn Nelson Robinson ,  Asghar Akber Peera

IPC: C09D5/00 ,  C07C213/02 ,  C07C205/15

CPC classification number: C07C201/12 ,  C07C213/02 ,  C08K5/17 ,  C07C205/15 ,  C07C215/18

Abstract: A method for preparing a compound having formula (II) wherein R1 and R2 independently are methyl or ethyl, or R1 and R2 combine to form a C5 or C6 cycloalkyl or cycloalkenyl group. The method includes a step of combining R1R2CHNO2, glutaraldehyde and an amine. The compound is useful in coating compositions and other applications for pH adjustment.

Abstract translation: 制备具有式（II）的化合物的方法，其中R 1和R 2独立地是甲基或乙基，或R 1和R 2结合形成C 5或C 6环烷基或环烯基。 该方法包括组合R1R2CHNO2，戊二醛和胺的步骤。 该化合物可用于涂料组合物和其它用于pH调节的应用中。

公开(公告)号：US08217180B2

公开(公告)日：2012-07-10

申请号：US12679382

申请日：2008-08-04

Applicant: Gary David Annis ,  Brenton Todd Smith

Inventor： Gary David Annis ,  Brenton Todd Smith

IPC: C07D261/04 ,  C07C233/00

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 with hydroxylamine in the presence of a base. The present invention also relates to novel compounds of Formula 2, useful as starting materials for the aforedescribed method.

Abstract translation: 公开了制备式1化合物的方法，其中R1是CHX2，CX3，CX2CHX2或CX2CX3; 每个X独立地为Cl或F; Z是任选取代的苯基; 且Q为苯基或1-萘基，各自如本公开所定义; 包括在碱的存在下使式2的化合物与羟胺接触。 本发明还涉及用作上述方法的起始原料的新的式2化合物。

公开(公告)号：US20120172634A1

公开(公告)日：2012-07-05

申请号：US13340448

申请日：2011-12-29

Applicant: Guangbin Dong ,  Robert H. Grubbs ,  Peili Teo ,  Zach K. Wickens

Inventor： Guangbin Dong ,  Robert H. Grubbs ,  Peili Teo ,  Zach K. Wickens

IPC: C07C29/143

CPC classification number: C07C29/143 ,  C07C29/03 ,  C07C29/14 ,  C07C45/30 ,  C07C201/12 ,  C07C47/27 ,  C07C49/225 ,  C07C33/22 ,  C07C33/20 ,  C07C33/18 ,  C07C33/46 ,  C07C47/273 ,  C07C31/125 ,  C07C47/02 ,  C07C205/19

Abstract: The disclosure provides a dual-catalysis system for direct conversion of olefins to alcohols. The cooperative catalytic system contains one oxidizing catalyst and one transfer-hydrogenation catalyst. A wide variety of olefins, including aromatic and aliphatic olefins, can be used as the reactant. The transformation proceeds with anti-Markovnikov selectivity, and in some aspects provides primary alcohols as major products. The disclosure further provides a system for oxidation of olefins with anti-Markovnikov selectivity.

Abstract translation: 本公开提供了用于将烯烃直接转化成醇的双催化体系。 合作催化体系含有一种氧化催化剂和一种转移氢化催化剂。 可以使用多种烯烃，包括芳族和脂族烯烃，作为反应物。 转化进行反马尔科夫尼科夫选择性，并且在一些方面提供伯醇作为主要产物。 本公开进一步提供了具有抗马尔科夫尼科夫选择性的烯烃氧化体系。

公开(公告)号：US20120130113A1

公开(公告)日：2012-05-24

申请号：US13387598

申请日：2010-07-27

Applicant: Omar M. Yaghi ,  Alexander U. Czaja ,  Bo Wang ,  Zheng Lu

Inventor： Omar M. Yaghi ,  Alexander U. Czaja ,  Bo Wang ,  Zheng Lu

IPC: C07C253/30 ,  C07C209/68 ,  C07C2/00 ,  C07C201/12 ,  C07C17/26

CPC classification number: C07C201/12 ,  C07C1/321 ,  C07C17/263 ,  C07C209/68 ,  C07C253/30 ,  C07C2523/72 ,  C07C2531/28 ,  C07C15/14 ,  C07C25/18 ,  C07C211/50 ,  C07C255/51 ,  C07C205/06

Abstract: The disclosure provides methods for the use of open metal frameworks to catalyze coupling reactions.

Abstract translation: 本公开提供了使用开放金属框架催化偶联反应的方法。

公开(公告)号：US20120123120A1

公开(公告)日：2012-05-17

申请号：US13263333

申请日：2010-04-01

Applicant: Nagichettiar Satyamurthy ,  Jorge R. Barrio

Inventor： Nagichettiar Satyamurthy ,  Jorge R. Barrio

IPC: C07D233/38 ,  C07C41/22 ,  C07C201/12 ,  C07D405/12 ,  C07C227/16 ,  C07D413/12 ,  C07D263/18 ,  C07C17/361 ,  C07D319/06

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.

Abstract translation: 显示了用芳族亲核取代反应的前体作为芳族环上的给电子基团和吸电子基团取代的苯基碘鎓衍生物衍生物。 碘鎓叶立德基团被诸如卤素离子的亲核试剂取代，得到相应的卤代芳基衍生物。 无载体添加的[F-18]氟化物离子专门代替这些衍生物中的碘鎓内鎓盐部分，并提供高比活性F-18标记的氟衍生物。 已经合成了保护的左旋多巴-6-碘鎓叶立德衍生物作为制备无载体添加的6- [F-18]氟-L-多巴的前体。 该L-多巴胺衍生物中的碘鎓叶立德碱通过无载体添加的[F-18]氟离子被亲核取代，得到[F-18]氟中间体，其在酸水解时产生6- [F-18]氟 -L-多巴

公开(公告)号：US08124813B2

公开(公告)日：2012-02-28

申请号：US12665066

申请日：2008-06-11

Applicant: Thomas-Norbert Müller ,  Michael Dockner

Inventor： Thomas-Norbert Müller ,  Michael Dockner

IPC: C07C43/315 ,  C07C45/42 ,  C07C41/50

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

Abstract: The invention relates to a novel process for preparing 2-phenoxyacetals and the corresponding 2-phenoxycarbaldehydes. These compounds are important intermediates for the preparation of active pharmaceutical ingredients.

Abstract translation: 本发明涉及一种制备2-苯氧基缩醛和相应的2-苯氧基羰基醛的新方法。 这些化合物是制备活性药物成分的重要中间体。

公开(公告)号：US20120004424A1

公开(公告)日：2012-01-05

申请号：US12782706

申请日：2010-05-18

Applicant: GUOFU ZHONG ,  BIN TAN ,  XUAN ZHANG ,  PEI JUAN CHUA

Inventor： GUOFU ZHONG ,  BIN TAN ,  XUAN ZHANG ,  PEI JUAN CHUA

IPC: C07C205/45 ,  C07D307/46 ,  C07D333/22

CPC classification number: C07D333/22 ,  C07C201/12 ,  C07D307/46 ,  C07D401/06 ,  C07C205/45

Abstract: Disclosed is a process of carrying out a Michael reaction with recovery of the catalyst, where a compound of formula (1): is reacted with a compound of formula (2): in the presence of a catalyst of formula (4): where the compounds of formulae (1) and (2) undergo a Michael reaction.

Abstract translation: 公开了一种通过回收催化剂进行迈克尔反应的方法，其中式（1）化合物与式（2）化合物在式（4）的催化剂存在下反应：其中 式（1）和（2）的化合物经历迈克尔反应。

公开(公告)号：US08058471B2

公开(公告)日：2011-11-15

申请号：US12376803

申请日：2007-08-08

Applicant: Susumu Amano ,  Akio Fujii ,  Shohei Yamamoto ,  Masaru Mitsuda

Inventor： Susumu Amano ,  Akio Fujii ,  Shohei Yamamoto ,  Masaru Mitsuda

IPC: C07C59/00 ,  C07C65/21

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: 本发明的目的在于提供一种光学活性羟基羧酸衍生物的制造方法，该方法是制备药物，农药，化学品等的重要中间体。 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反应，生成光学活性羟基羧酸衍生物。 根据本发明，可以安全有效地制备工业上有用的光学活性羟基羧酸衍生物。

公开(公告)号：US08049017B2

公开(公告)日：2011-11-01

申请号：US13039137

申请日：2011-03-02

Applicant: Joachim Rheinheimer ,  Wolfgang von Deyn ,  Joachim Gebhardt ,  Michael Rack ,  Rene Lochtman ,  Norbert Götz ,  Michael Keil ,  Matthias Witschel ,  Helmut Hagen ,  Ulf Miβlitz ,  Ernst Baumann

Inventor： Joachim Rheinheimer ,  Wolfgang von Deyn ,  Joachim Gebhardt ,  Michael Rack ,  Rene Lochtman ,  Norbert Götz ,  Michael Keil ,  Matthias Witschel ,  Helmut Hagen ,  Ulf Miβlitz ,  Ernst Baumann

IPC: C07D261/04

CPC classification number: C07C249/06 ,  C07C201/10 ,  C07C201/12 ,  C07C205/44 ,  C07C209/62 ,  C07C251/48 ,  C07C253/00 ,  C07C255/50 ,  C07C315/04 ,  C07C319/14 ,  C07D261/04 ,  C07D413/10 ,  C07C323/09 ,  C07C317/24 ,  C07C317/32 ,  C07C205/06 ,  C07C211/52

Abstract: A process is described for preparing isoxazoles of the formula I where the substituents are as defined below: R1 is hydrogen, C1-C6-alkyl, R2 is C1-C6-alkyl, R3, R4, R5 are hydrogen, C1-C6-alkyl, or R4 and R5 together form a bond, R6 is a heterocyclic ring, n is 0, 1 or 2; which comprises preparing an intermediate of the formula VI where R1, R3, R4 and R5 are as defined above, followed by halogenation, thiomethylation, oxidation and acylation to give compounds of the formula I. Also novel intermediates for preparing the compounds of the formula I and novel processes for preparing the intermediates are described.

Abstract translation: 描述了制备式I的异恶唑的方法，其中取代基如下所定义：R 1是氢，C 1 -C 6烷基，R 2是C 1 -C 6烷基，R 3，R 4，R 5是氢，C 1 -C 6 - 烷基 ，或R4和R5一起形成键，R6是杂环，n是0,1或2; 其包括制备式VI的中间体，其中R 1，R 3，R 4和R 5如上定义，然后进行卤化，硫甲基化，氧化和酰化，得到式I化合物。还有用于制备式I化合物的中间体 并描述了制备中间体的新方法。