- Bicyclo [2.2.2] octane - 1, 4 - dicarboxylic acid mono methyl ester synthesis method
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The invention relates to a synthetic method of an organic compound. The synthetic method of bicyclo-[2.2.2]octane-1,4-dicarboxylic acid monomethyl easter is as follows: firstly, adopting sodium hydride, DMSS and 1,2-dibromoethane to synthesize the intermediate I; secondly, adopting the intermediate I, sodium acetate, ammourea hydrochloride and alcohol to synthesize semicarbazon; thirdly, adopting potassium hydroxide, diethylene glycol and semicarbazon to synthesize target diacid; fourthly, adopting target diacid, thionyl chloride and methanol to synthesize target diester; and fifthly, adopting target diester, potassium hydroxide and 95% of methanol water solution to synthesize the target product monoester. The invention has reasonable synthetic process route, mild process conditions, environment friendly, easy operation, low raw material cost, high product yield and excellent purity, and is applicable to industrial production and satisfies the application requirement of each industry.
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Paragraph 0007; 0024; 0025; 0026; 0027; 0036; 0037
(2017/07/07)
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- POLYMERIZABLE COMPOUND AND OPTICAL ANISOTROPIC BODY
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PROBLEM TO BE SOLVED: To provide a polymerizable composition that causes few orientation defects when added to a polymerizable composition and making a film-like polymer, and is resistant to discoloration when put in a high temperature condition. SOLUTION: The present invention provides a compound illustrated by the formula (I-6), a polymerizable composition containing the compound, a polymer obtained by the polymerization of the composition, and an optical anisotropic body prepared with the polymer. SELECTED DRAWING: None COPYRIGHT: (C)2018,JPO&INPIT
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Paragraph 0202-0204
(2018/01/02)
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- Substituted pyrazolo-piperazines as casein kinase 1 δ/ε inhibitors
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The invention provides compounds of Formula (I): and pharmaceutically acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents.
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Page/Page column 527; 528
(2016/03/19)
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- Design and synthesis of novel 19F-amino acid: A promising 19F NMR label for peptide studies
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Novel aliphatic 19F-substituted amino acid was designed as a 19F NMR label for peptide studies. The synthesis was performed in 11 steps and 9% overall yield from a commercially available starting material. The key transformation was a decarboxylative fluorination of an aliphatic carboxylic acid with XeF2 in C6F6.
- Bandak, Dmytro,Babii, Oleg,Vasiuta, Roman,Komarov, Igor V.,Mykhailiuk, Pavel K.
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supporting information
p. 226 - 229
(2015/03/05)
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- COMBINATIONS OF HEPATITIS C VIRUS INHIBITORS
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The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.
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Page/Page column 467; 468
(2015/02/02)
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- Discovery of functionalized bisimidazoles bearing cyclic aliphatic-phenyl motifs as HCV NS5A inhibitors
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This Letter describes the discovery of a number of functionalized bisimidazoles bearing a cyclohexylphenyl, piperidylphenyl, or bicyclo[2,2,2]octylphenyl motif as HCV NS5A inhibitors. Compounds 2c, 4b and 6 have demonstrated low single-digit nM potency in gt-1a replicon and double-digit pM potency in gt-1b replicon, respectively. Moreover, both 4b and 6 have, respectively, exhibited good oral bioavailability in rats with a favorable liver/plasma ratio of the drug concentration.
- Zhong, Min,Peng, Eric,Huang, Ningwu,Huang, Qi,Huq, Anja,Lau, Meiyen,Colonno, Richard,Li, Leping
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p. 5731 - 5737
(2015/01/08)
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- BICYCLO [2.2.2] ACID GPR120 MODULATORS
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The present invention provides compounds of Formula (I) or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be use
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Paragraph 00189
(2014/10/15)
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- SPIRO AZETIDINE ISOXAZOLE DERIVATIVES AND THEIR USE AS SSTR5 ANTAGONISTS
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Provided is a compound represented by the following formula (1) or a salt thereof, which has an SSTR5 antagonistic action: wherein each symbol has the same definition as in the specification.
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Paragraph 1268; 1287
(2014/09/29)
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- BRIDGED BICYCLIC COMPOUNDS FOR THE TREATMENT OF BACTERIAL INFECTIONS
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Novel bridged bicyclic compounds are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antibacterial agents. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating bacterial infections and associated diseases and conditions.
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Page/Page column 64
(2013/03/26)
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- SUBSTITUTED DIAMINOCARBOXAMIDE AND DIAMINOCARBONITRILE PYRIMIDINES, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH
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Provided herein are Diaminopyrimidine Compounds having the following structures: wherein R1, R2, R3, and R4 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidine Compound, and methods for treating or preventing liver fibrotic disorders or a condition treatable or preventable by inhibition of a JNK pathway.
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Page/Page column 135
(2012/11/07)
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- NOVEL AMIDE AND AMIDINE DERIVATIVES AND USES THEREOF
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The present invention relates to inhibitors of 11-β-hydroxysteroid dehydrogenase type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.
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Page/Page column 32
(2010/11/03)
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- Discovery of a potent, selective, and orally efficacious pyrimidinooxazinyl bicyclooctaneacetic acid diacylglycerol acyltransferase-1 inhibitor
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Inhibition of DGAT-1 is increasingly seen as an attractive mechanism with the potential for treatment of obesity and other elements of the metabolic syndrome. We report here a bicyclooctaneacetic acid derivative in the pyrimidinooxazine structural class o
- Birch, Alan M.,Birtles, Susan,Buckett, Linda K.,Kemmitt, Paul D.,Smith, Graham J.,Smith, Tim J. D.,Turnbull, Andrew V.,Wang, Steven J. Y.
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experimental part
p. 1558 - 1568
(2010/01/07)
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- HETEROBICYCLIC METALLOPROTEASE INHIBITORS
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The present invention relates generally to heterobicyclic containing pharmaceutical agents, and in particular, to heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic metalloprotease inhibiting compounds that exhibit an increased potency in relation to currently known metalloprotease inhibitors.
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Page/Page column 177-178
(2008/12/05)
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- HETEROBICYCLIC METALLOPROTEASE INHIBITORS
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The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic MMP- 13 inhibiting compounds, that exhibit an increased potency in relation to currently known MMP- 13 inhibitors.
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Page/Page column 164-165
(2008/06/13)
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- Adenosine receptor antagonists and methods of making and using the same
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The invention is based on the discovery that compounds of Formula I are unexpectedly highly potent and selective inhibitors of the adenosine A1receptor. Adenosine A1antagonists can be usefull in the prevention and/or treatment of numerous diseases, including cardiac and circulatory disorders, degenerative disorders of the central nervous system, respiratory disorders, and many diseases for which diuretic treatment is suitable. In one embodiment, the invention features a compound of formula I: wherein: R3is an optionally substituted bicyclic, tricylic, or pentacyclic group selected from: ?and wherein R1, R2, R6, X1, X2, and Z are as described in the specification.
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Page/Page column 52
(2008/06/13)
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- The synthesis of [2.2.2]bicyclooctane and [3.1.1]bicycloheptane based amino acids as constrained glutamate analogues
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A novel [2.2.2]bicyclooctane analogue of glutamic acid was synthesised using a modification of the Corey-Link amino acid synthesis. A related [3.1.1]bicycloheptane was prepared by cyclising a symmetrical 4,4- disubstituted cyclohexanone.
- Richard Baker,Hancox, Timothy C.
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p. 781 - 784
(2007/10/03)
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- Rodlike molecules by Kolbe electrolysis
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A new short and simple pathway to rigid, rod-shaped hydrocarbon skeletons, in particular of the oligo-bicyclo[2.2.2]octane type, is described. The key step consists of an electrochemical C-C bond coupling reaction between bridgehead positions of bi- and tricyclic carboxylic acids. Functional groups can be retained, they influence the yield of the C-C bond connection. In this way, otherwise difficult or laborious syntheses are shortened, and rigid, non-collapsable nano size spacer units are easily available. The optimized electrochemical procedures are described in detail.
- Nuding,V?gtle,Danielmeier,Steckhan
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- Decarboxylation of Bridgehead Carboxylic Acids by the Barton Procedure
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Reductive decarboxylation of a series of bicyclic and polycyclic acids in which the carboxyl group is attached to the bridgehead position has been investigated.Conversion of the acids into thiohydroxamic esters occurs via reaction of the derived acid chlorides with N-hydroxypyridine-2-thione.Decomposition of the esters proceeds smoothly in boiling benzene in the presence of 1-butyl mercaptan to give the reduced product in high yield.The procedure appears to be generally applicable, and is unaffected by functional groups such as esters and acetals.
- Della, Ernest W.,Tsanaktsidis, John
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p. 2061 - 2066
(2007/10/02)
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- Polar Substituent Effects on 19F Chemical Shifts of Aryl and Vinyl Fluorides: A Fluorine-19 Nuclear Magnetic Resonance Study of Some 1,1-Difluoro-2-(4-substituted-bicyclooct-1-yl)ethenes
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An extensive series of 1,1-difluoro-2-(4-substituted-bicyclooct-1-yl)ethenes (2) covering a diverse range of substituents ( X = H, NO2, CN, CF3, COOCH3, F, Cl, Br, OCH3, C6H5, C2H, C2Si(CH3)3, CH3, and C(CH3)3) have been synthesized and their 19F N
- Adcock, William,Kok, Gaik B.
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p. 1079 - 1087
(2007/10/02)
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