- PALLADIUM CATALYZED SYNTHESIS OF NEW BICYCLOHEPT-2-ENE-CARBON MONOXIDE COPOLYMERS
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New cis, exo bicycloheptene-carbon monoxide copolymers, initiated by H or by a hydrocarbyl group and terminated by a χ-lactone with exocyclic double bond, are prepared at atmospheric pressure under the catalytic action of a palladium(0) complex.
- Roberto, Dominique,Catellani, Marta,Chiusoli, Gian Paolo
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- METHOD FOR PRODUCING NORBORNANE DICARBOXYLIC ACID
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The present invention relates to a method for producing norbornane carboxylic acid, and more specifically, to a method for producing norbornane carboxylic acid, which comprises a step for reacting cyclopentadiene obtained by thermal decomposition of dicyclopentadiene with maleic anhydride. The production method according to the present invention utilizes dicyclopentadiene, has excellent reaction efficiency, and has an industrially useful whole reaction process, and thus it is possible to mass-produce the norbornane dicarboxylic acid with high yield and the norbornane dicarboxylic acid can be applied to various industrial fields.COPYRIGHT KIPO 2018
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Paragraph 0092; 0099; 0100
(2018/07/28)
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- METHOD FOR PRODUCING BICYCLO[2.2.1]HEPTANE-2,3-DIYLDIMETHANOL
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The present invention refers to bicyclo [2. 2. 1] Heptane - 2, 3 - manufacturing method relates to the d methanol which will be a d, more particularly claw pen hit diene between d and reacting maleic anhydride with pen hit diene obtained by pyrolysis cycles including a number bath is formed on the bicyclo [2. 2. 1] Heptane - 2, 3 - to the d methanol which will be a d manufacturing method are disclosed. The present invention according to manufacturing method is that by the claw pen hit diene between d, reaction efficiency is superior, since the whole reaction process industrially useful bicyclo [2. 2. 1] Heptane - 2, 3 - [...] high yield can be mass produced, industrially nephrophathy intensity applications. (by machine translation)
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Paragraph 0107-0108
(2018/07/28)
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- PROCESS FOR PREPARING BENZISOTHIAZOL-3-YL-PEPERAZIN-L-YL-METHYL-CYCLO HEXYL-METHANISOINDOL-1,3-DIONE AND ITS INTERMEDIATES
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The present invention discloses process for preparing benzisothiazol-3-yl- piperazin-l-yl-methyl-cyclo hexyl-methanisoindol-l,3-dione and intermediates thereof.
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Page/Page column 29
(2013/08/28)
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- ENDO-METHYLENE HEXAHYDROPHTHALIC ANHYDRIDE AND PRODUCTION METHOD THEREOF
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The present invention belongs to the field of organic chemical synthesis, and discloses hexahydro-3,6-methanophthalic anhydride and a method of producing the same. The method uses maleic anhydride and mixed C5s as raw materials, generates Nadic anhydride by absorbing cyclopentadiene with maleic anhydride directly at a temperature of 0-5°C, and crystallizes to obtain a pure product; and a Cu-Ni/ZnO-ZrO2 or Co-Ni/ZnO-ZrO2 catalyst is added to the generated Nadic anhydride, carrying out a catalytic hydrogenation reaction in a high-pressure autoclave for 4-6 hours at a temperature of 100-140°C and under a hydrogen pressure of 1-4 MPa, the catalyst is filtered after cooling, and reduced pressure distilling to obtain the hexahydro-3,6-methanophthalic anhydride. Compared with the prior art, the present invention prepares the Nadic anhydride by using mixed C5s, an inexpensive by-product of ethylene, as a raw material, and further synthesizes hexahydro-3,6-methanophthalic anhydride while obtaining a chemical raw material de-cyclized C5s at the same time, enhances the in-depth processing of mixed C5s, and can be used widely in industrial production.
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Page/Page column 4-5
(2012/09/21)
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- NOVEL LIQUID TETRACARBOXYLIC DIANHYDRIDES AND PROCESS FOR THE PREPARATION THEREOF
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The invention relates to a tetracarboxylic dianhydride represented by the following formula (1). [In formula (1) R1, R2, R3 and R4 each independently represent an alkyl group having from 1 to 5 carbon atoms, m represents a number from 1 to 30, all of the silicon atoms bonding to the norbornane rings are in an exo-configuration with respect to the norbornane rings, and all of the dicarboxylic anhydride groups bonding to the norbornane rings are in an exo-configuration with respect to the norbornane rings.]
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- METHOD OF SEPARATING STEREOISOMERS OF NORBORNENE, DICARBOXYLIC ACID HAVING NORBORNANE STRUCTURE, OR DERIVATIVE THEREOF
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A method of efficiently extracting a high-purity stereoisomer from a mixture comprising the endo isomer and the exo isomer of a dicarboxylic acid having a norbomene or norbomane structure, or a derivative thereof. The present invention relates to a method of separating the endo isomer and the exo isomer of a dicarboxylic acid represented by a general formula (1) or (2) or a derivative thereof, and includes the step of stirring and mixing a mixture comprising mainly the endo isomer of the dicarboxylic acid represented by the general formula (1) or (2) or a derivative thereof, and the exo isomer of the dicarboxylic acid represented by the general formula (1) or (2) or a derivative thereof, with a basic compound and a solvent. (wherein, R1 to R8 represent a hydrogen atom, methyl group, ethyl group, or butyl group), (wherein, R'1 to R'10 represent a hydrogen atom, methyl group, ethyl group, or butyl group)
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Page/Page column 19
(2008/06/13)
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- Highly efficient nickel-catalyzed cross-coupling of succinic and glutaric anhydrides with organozinc reagents
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A nickel-catalyzed alkylation of succinic and glutaric anhydrides with alkyl- and arylzinc reagents has been developed. A dramatic olefin effect has been investigated resulting in the identification of several styrene-based promoters which show pronounced enhancements in reaction rate. The substrate scope with respect to electrophilic and nucleophilic coupling partners has been examined and found to be remarkably broad, allowing for rapid introduction of molecular complexity through the use of functionalized coupling partners. Regioselective alkylation of an unsymmetrical succinic anhydride and a profound effect of pendent coordinating olefins on reaction rate suggest a mechanism involving discrete oxidative addition of the nickel complex into the cyclic anhydride followed by a transmetalation event.
- Bercot, Eric A.,Rovis, Tomislav
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p. 247 - 254
(2007/10/03)
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- Preparation and structure of di-exo-condensed norbornane heterocycles
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Cyclization of di-exo-aroylnorbornanecarboxylic acid with bidentate nucleophiles (hydrazine, o-phenylenediamine, o-aminophenol, alkylenediamines, and amino alcohols) yielded heterotri-, tetra-, and pentacycles. Their structures were established by means o
- Miklos, Ferenc,Hetenyi, Anasztazia,Sohar, Pal,Stajer, Geza
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p. 839 - 847
(2007/10/03)
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- Protein phosphatase 2A inhibition and circumvention of cisplatin cross-resistance by novel TCM-platinum anticancer agents containing demethylcantharidin
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The structurea€"activity requirement of the PP2A-inhibiting demethylcantharidin for the circumvention of cisplatin cross-resistance demonstrated by the novel TCMa€"Pt compounds is discussed. Novel TCM-platinum compounds [Pt(C8H8O5)(NH 2R)2] 1-5, derived from integrating demethylcantharidin, a modified component from a traditional Chinese medicine (TCM) with a platinum moiety, possess anticancer and protein phosphatase 2A inhibition properties. The compounds are able to circumvent cisplatin resistance by apparently targeting the DNA repair mechanism. Novel isosteric analogues [Pt(C9H 10O4)(NH2R)2] A and B, devoid of PP2A-inhibitory activity, were found to suffer from an enhanced DNA repair and were cross-resistant to cisplatin. The results advocate a well-defined structure-activity requirement associating the PP2A-inhibiting demethylcantharidin with the circumvention of cisplatin cross-resistance demonstrated by TCM-Pt compounds 1-5.
- To, Kenneth K.W.,Wang, Xinning,Yu, Chun Wing,Ho, Yee-Ping,Au-Yeung, Steve C.F.
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p. 4565 - 4573
(2007/10/03)
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- Decarbonylative cross-coupling of cyclic anhydrides: Introducing stereochemistry at an sp3 carbon in the cross-coupling event
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Treatment of cyclic anhydrides with stoichiometric amounts of nickel-neocuproine complex generates alkylcarboxylato-nickelalactones upon extrusion of CO. These metalacycles undergo cross-coupling with arylzinc reagents. The generated CO is sequestered in situ by a nickel-dppb complex. The overall sequence effects a secondary sp3(electrophile)-sp2(nucleophile) cross-coupling and allows for control of stereochemistry during the bond-forming event. Copyright
- O'Brien, Erin M.,Bercot, Eric A.,Rovis, Tomislav
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p. 10498 - 10499
(2007/10/03)
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- Succinimide derivatives. II. Synthesis and antipsychotic activity of N- [4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]1,2-cis- cyclohexanedicarboximide (SM-9018) and related compounds
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Cyclic imides bearing ω-(4-benzisothiazol-3-yl-1-piperazinyl)alkyl moieties were synthesized and tested for antipsychotic activity. The in vitro binding affinities of these compounds were examined for dopamine 2 (D2) and serotonin 2 (5-HT2) receptor sites. Structure-activity relationships within these series are discussed. One of these compounds, N-[4-[4-(1,2- benzisothiazol-3-yl)-1-piperazinyl]butyl]-1,2-cis-cyclohexanedicarboximide (SM-9018), was found to be more potent and more selective in vivo than tiospirone in its antipsychotic activity. SM-9018 (17) is currently undergoing clinical evaluation as a selective antipsychotic agent.
- Ishizumi,Kojima,Antoku,Saji,Yoshigi
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p. 2139 - 2151
(2007/10/03)
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- Synthesis and anxiolytic activity of N-substituted cyclic imides (1R*,2S*3R*,4S*)-N-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,3-b icyclo[2.2.1]heptanedicarboxime (Tandospirone) and related compounds
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A series of cyclic imides bearing a ω-(4-aryl and 4-heteroaryl-1-piperazinyl)alkyl moieties was synthesized and tested in vivo for anxiolytic activity. The in vitro binding affinities of these compounds were also examined for 5-HT(1A) receptor sites. Structure-activity relationships within these series are discussed. One of these compounds, (1R*,2S*,3R*,4S*)-N-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,3- bicyclo[2.2.1]heptanedicarboximide (1: tandospirone), was found to be equipotent with buspirone in its anxiolytic activity and more anxio-selective than buspirone and diazepam. Tandospirone (1) is currently undergoing clinical evaluation as a selective anxiolytic agent.
- Ishizumi,Kojima,Antoku
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p. 2288 - 2300
(2007/10/02)
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- Novel Synthesis of Five- and Six-Membered Spiro γ-Lactones in Rigid Bicyclic Systems
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The reaction of bis(bromomagnesio)alkanes with bridged tricyclic endo- and exo-dicarboxylic anhydrides and their dihydro derivatives provides a general and versatile route to corresponding tricyclic spiro γ-butanolides.Futher extension of this methodology to the dianhydride of bicyclooctene showed appreciable regioselectivity.The subsequent transformation of spiro γ-lactones into 4-spiro-2-butenolides by retro-Diels-Alder reaction has provided a simple and convenient synthesis of these molecules.Proton and 13C NMR spectra are reported for most of the compounds.
- Cannone, Persephone,Belanger, Denis,Lemay, Gilles
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p. 3953 - 3959
(2007/10/02)
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