- A Skeletal Rearrangement of γ-(Acyloxy)-β-keto Phosphonates: Studies on the Formation of 2(3H)-Furanones
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When treated with sodium hydride in dimethoxyethane, some γ-(acyloxy)-β-keto phosphonates react to give 2(3H)-furanones via an unexpected rearrangement which proceeds with carbon-carbon bond formation.Several possible mechanisms for this transformation have been tested through crossover experiments, rearrangement of an isotopically labeled substrate, and synthesis of a model intermediate.Results from these experiments allow elimination of several potential reaction pathways from further consideration and suggest a focus for future studies.
- Roussis, Vassilios,Gloer, Katherine B.,Wiemer, David F.
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- The oxidative cleavage of trans-1,2-cyclohexanediol with O2: Catalysis by supported Au nanoparticles
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This paper reports on the catalytic oxidative cleavage of trans-1,2-cyclohexanediol with air, catalysed by supported Au NPs, as one of the steps of a new adipic acid synthesis process. Catalysts proved to be active, with a moderate cyclohexanediol conversion and selectivity to adipic acid close to 70%. The reaction network included several steps in sequence, amongst which the key one is the oxidation of the diol into 2-hydroxycylohexanone, which is then oxidised by air – even in the absence of a catalyst – to adipic acid and lesser amounts of lighter acids, i.e. glutaric and succinic acids. The oxidation of the second hydroxyl moiety in the diol would lead to the formation of 1,2-cyclohexanedione. The latter, however, is rapidly transformed into several by-products, especially glutaric acid, under the basic conditions which are necessary for allowing the reaction to occur at an acceptable rate. With Au-based catalysts, this undesired reaction occurs much more slowly than with the previously investigated Ru hydroxide catalysts. The nature of the support, either TiO2 or MgO, also affected catalytic performance; the best performance was shown by the Au/MgO catalyst which, however, suffered from a remarkable deactivation, found to be due to both the increase in NPs size and the formation of carbonaceous residua on the catalyst surface.
- Solmi, Stefania,Rozhko, Elena,Malmusi, Andrea,Tabanelli, Tommaso,Albonetti, Stefania,Basile, Francesco,Agnoli, Stefano,Cavani, Fabrizio
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- Volution lactone compound and synthesis method and application thereof
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The invention discloses a volution lactone compound. The chemical structural formula of the volution lactone compound is shown in the specification. A preparing method of the volution lactone compound includes the steps that (1) cyclopentanone serves as a raw material and is subjected to a cyanohydrintion reaction, then cyano groups are hydrolyzed and esterified, and hydroxyl-cyclopentanecarboxylic acid ethyl ester is obtained; (2) a sulfonation reaction is carried out; (3) a butt joint ring formation reaction is carried out; (4) an alkylation reaction is carried out, wherein the cyclizing product obtained in the step (3), a reaction solvent and a catalyst are mixed, 3-bromopropylene is added into the mixed liquid, the solvent is removed in a pressure-reduction mode after reacting, water and benzene are added, extracting and layering are carried out, an organic phase substance is obtained, solvent pressure-reduction removing and filtering are carried out, and the final product volution lactone compound is obtained. The volution lactone compound has the advantage that a pesticide good in pest killing effect, long in lasing period and low in toxicity is obtained.
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Paragraph 0051-0052
(2017/05/12)
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- Anesthetic compounds and related methods of use
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Provided herein are compounds according to formula (I): Provided herein is also a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and a method for providing anesthesia in a subject by administering such a pharmaceutical composition.
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Page/Page column 64
(2015/11/09)
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- N-Acyl-N'-(pyridin-2-yl) Ureas and Analogs Exhibiting Anti-Cancer and Anti-Proliferative Activities
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Described are compounds of Formula 1 which find utility in the treatment of cancer, autoimmune diseases and metabolic bone disorders through inhibition of c-FMS (CSF-1R), c-KIT, and/or PDGFR kinases. These compounds also find utility in the treatment of other mammalian diseases mediated by c-FMS, c-KIT, or PDGFR kinases.
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Paragraph 0260
(2014/09/29)
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- N-Acyl-N'-(pyridin-2-yl) Ureas and Analogs Exhibiting Anti-Cancer and Anti-Proliferative Activities
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Described are compounds of Formula I which find utility in the treatment of cancer, autoimmune diseases and metabolic bone disorders through inhibition of c-FMS (CSF-1R), c-KIT, and/or PDGFR kinases. These compounds also find utility in the treatment of other mammalian diseases mediated by c-FMS, c-KIT, or PDGFR kinases.
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Paragraph 0394
(2014/09/30)
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- ANESTHETIC COMPOUNDS AND RELATED METHODS OF USE
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Provided herein are compounds according to formula (I): Provided herein is also a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and a method for providing anesthesia in a subject by administering such a pharmaceutical composition.
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Paragraph 00199
(2013/07/25)
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- NON-SYSTEMIC TGR5 AGONISTS
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Compounds of structure (I), or a stereoisomer, tautomer, pharmaceutically acceptable salt or prodrug thereof, wherein R1, R2, R3, R4, R8, R9, R10, R11, R12, A1, A2, X, Y and Z are as defined herein. Uses of such compounds as TGR5 antagonists and for treatment of various indications, including Type II diabetes meletus are also provided.
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- Bradykinin B1 receptor antagonists: An α-hydroxy amide with an improved metabolism profile
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A series of carbo- and heterocyclic α-hydroxy amide-derived bradykinin B1 antagonists was prepared and evaluated. A 4,4-difluorocyclohexyl α-hydroxy amide was incorporated along with a 2-methyl tetrazole in lieu of an oxadiazole to afford a suitable compound with good pharmacokinetic properties, CNS penetration, and clearance by multiple metabolic pathways.
- Kuduk, Scott D.,Chang, Ronald K.,DiPardo, Robert M.,Di Marco, Christina N.,Murphy, Kathy L.,Ransom, Richard W.,Reiss, Duane R.,Tang, Cuyue,Prueksaritanont, Thomayant,Pettibone, Douglas J.,Bock, Mark G.
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scheme or table
p. 5107 - 5110
(2009/05/26)
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- Oxazolones as potent inhibitors of 11β-hydroxysteroid dehydrogenase type 1
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2,5,5-Trisubstituted oxazolones were identified as potent inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The synthesis, structure-activity relationship and metabolic stability of these compounds are presented.
- Sutin, Lori,Andersson, Soeren,Bergquist, Lars,Castro, Victor M.,Danielsson, Eva,James, Stephen,Henriksson, Martin,Johansson, Lars,Kaiser, Christina,Flyren, Katarina,Williams, Meredith
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p. 4837 - 4840
(2008/02/11)
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- l-HYDROXYCYCLOALKANECARBOXAMIDE DERIVATIVES AS BRADYKININ ANTAGONISTS
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α-Hydroxycycloalkanecarboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, wherein formula (a) is a single or double bond; Rl, R2 and R3 are each independently selected from H, halogen and OH; or Rl and R2 attached to the same carbon atom together represent oxo; R4 is H or methyl; R5 is Cl or F; R6 is selected from -CO2-C1-4alkyl, -O-C1-4alkyl, -O- C1-4haloalkyl, 2-methyltetrazol-5-yl, 5-methyl l,2,4-oxadiazol-3-yl, 3-methyl-1,2,4-oxadiazol-5-yl, 5-halomethyl-l,2,4-oxadiazol-3-yl, 3-halomethyl- l,2,4-oxadiazol-5-yl, tetrazol-5-yl, 5-halomethyl-l,2,3-triazolyl, and 5-methyl-l ,2,3-triazolyl; R7 and R8 are each independently Cl or F; and n is 0 or 1, are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
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Page/Page column 23-25
(2008/06/13)
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- Spirodiclofen and spiromesifen - Novel acaricidal and insecticidal tetronic acid derivatives with a new mode of action
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The broad spectrum acaricides spirodiclofen (BAJ2740, trade name: Envidor) and spiromesifen (BSN2060, trade name: Oberon) with an additional excellent activity against whiteflies, both belong to the new chemical class of tetronic acid derivatives discovered at Bayer CropScience during the 1990s. The discovery process starting from herbicidal PPO (protoporphyrinogen oxidase) chemistry, the synthetic routes leading to the products, and some insight into process development of central intermediates is given. Spirodiclofen and spiromesifen have a new mode of action (interference with lipid biosynthesis), show no cross-resistance to any resistant mite or whitefly field population and are therefore valuable tools for resistance management.
- Bretschneider, Thomas,Benet-Buchholz, Jordi,Fischer, Reiner,Nauen, Ralf
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p. 697 - 701
(2007/10/03)
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- A Ring Contraction Induced by Hydrogenperoxide
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2-Amino-7a-carbamoyl-3a-hydroxy-3a,4,5,6,7,7a-hexahydro-benzoxazole (1) and hydrogenperoxide rearrange to 2'-amino-cyclopentanespiro-5'-oxazolin-4'-one (5). 5 and aniline hydrochloride form the phenylaminoderivative 6, 5 and 2,5-dichlorophenylhydrazine hydrochloride form the 2,5-dichlorophenylhydrazinederivative 7. 5 and hydrochloric acid afford cyclopentanespiro-5'-oxazolidin-2',4'-dione (8).Hydrolysis of 5 or 8 furnish 1-hydroxy-cyclopentane-carboxylic acid (9).
- Bischoff, Christian,Gruendemann, Egon,Schroeder, Edith
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p. 184 - 186
(2007/10/02)
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