- A new technique to prepare 9-oxofluorene-2-carboxylic acid
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9-Oxofluorene-2-carboxylic acid has been obtained with a yield as high as 98.5%, following a new procedure with easy product extraction, based on the reaction of 2-acetylfluorene with sodium dichromate in acetic acid.
- Salmeron-Valverde,Robles-Martinez,Campos-Medina,Zehe
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Read Online
- Method for synthesizing fluorenone ketone compound through molecular oxygen oxidation in water phase
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Aiming at the technical problems that in the prior art a method for synthesizing a fluorenone ketone compound has organic solvent pollution and byproducts can be generated, the invention provides a method for synthesizing a fluorenone ketone compound through molecular oxygen oxidation in a water phase. The method comprises the following steps: by taking a fluorenone compound as a substrate, dispersing into an alkali solution, and at 40-120 DEG C, in the presence of oxygen, and with a water-soluble transition metal compound as a catalyst, stirring to carry out reactions, thereby obtaining the fluorenone ketone compound. By adopting the method, molecular oxygen is adopted as an oxidant, and water is adopted as a solvent, so that an organic solvent is avoided, and the problem that multiple byproducts are generated because of peroxidation can be avoided.
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Paragraph 0067; 0069
(2019/08/20)
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- With Wnt signal path to inhibit the active heterocyclic compounds (by machine translation)
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The invention relates to a signal path with Wnt inhibiting activity of a heterocyclic compound, including the compound and its pharmaceutically acceptable salt, various isotope, various isomers or various crystal structure, having the general formula I of the structure shown in: the invention relates to a compound and its joint application composition can effectively inhibit the Wnt signal path, can be used for the treatment or prevention of a disorder associated with a Wnt signal path. (by machine translation)
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Paragraph 0102-0104; 0109-0110
(2017/08/15)
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- Design, synthesis, and evaluation of novel porcupine inhibitors featuring a fused 3-ring system based on the ‘reversed’ amide scaffold
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The Wnt signaling pathway is an essential signal transduction pathway which leads to the regulation of cellular processes such as proliferation, differentiation and migration. Aberrant Wnt signaling is known to have an association with multiple cancers. Porcupine is an enzyme that catalyses the addition of palmitoleate to a serine residue in Wnt proteins, a process which is required for the secretion of Wnt proteins. Here we report the synthesis and structure–activity-relationship of the novel porcupine inhibitors based on a ‘reversed’ amide scaffold. The leading compound 53 was as potent as the clinical compound LGK974 in a cell based STF reporter gene assay. Compound 53 potently inhibited the secretion of Wnt3A, therefore was confirmed to be a porcupine inhibitor. Furthermore, compound 53 showed excellent chemical and plasma stabilities. However, the clearance of compound 53 in liver microsomal tests was moderate to high, and the solubility of compound 53 was suboptimal. Collective efforts toward further optimization of this novel tricyclic template to develop better porcupine inhibitors will be subsequently undertaken and reported in due course.
- Xu, Zhixiang,Xu, Xiangxiang,O'Laoi, Ruadhan,Ma, Haikuo,Zheng, Jiyue,Chen, Shuaishuai,Luo, Lusong,Hu, Zhilin,He, Sudan,Li, Jiajun,Zhang, Hongjian,Zhang, Xiaohu
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p. 5861 - 5872
(2016/10/30)
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- Polymeric Reagents Comprising a Terminal Vinylic Group and Conjugates Formed Therefrom
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The present invention provides conjugates having a degradable linkage and polymeric reagents useful in preparing such conjugates. Methods of making polymeric reagents and conjugates, as well as methods for administering conjugates and compositions, are also provided.
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- Optimized liquid-phase oxidation
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Disclosed is an optimized process and apparatus for more efficiently and economically carrying out the liquid-phase oxidation of an oxidizable compound. Such liquid-phase oxidation is carried out in a bubble column reactor that provides for a highly effic
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Page/Page column 39-41
(2008/06/13)
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- Optimized liquid-phase oxidation
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Disclosed is an optimized process and apparatus for more efficiently and economically carrying out the liquid-phase oxidation of an oxidizable compound. Such liquid-phase oxidation is carried out in a bubble column reactor that provides for a highly effic
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Page/Page column 39-41
(2008/06/13)
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- Antithrombotic agents
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This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a prodrug thereof, as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
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- Liquid-Phase Catalytic Oxidation of 2,4-Dimethylbiphenyl
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2,4-Dimethylbiphenyl synthesized by alkylalion of m-xylene with cyclohexanol and subsequent dehydrogenation was oxidized catalytically in the liquid phase to 2,4-biphenyldicarboxylic acid. The effects of temperature, the catalyst, and initial concentrations of reactants on the rate and efficiency of the process were studied.
- Koshel',Lebedeva,Rudkovskii,Krestinina,Koshel',Danilova
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- TRINITRO-9-OXOFLUORENECARBOXAMIDES AS CHIRAL ELECTRON ACCEPTORS
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Trinitrofluorenecarboxamides, labeled with optically active α-phenylethylamine and some of its derivatives, were synthesized in a continuation of researches into new chiral electron acceptors of the nitrofluorene series.Their possible use as chiral acceptors in the resolution of compounds into enantiomers by chromatographic separation of diastereomeric charge-transfer complexes was investigated.
- Il'ina, I.G.,Ivanova, E.V.,Sokolova, E.L.,Mikhalev, O.V.
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p. 266 - 269
(2007/10/02)
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- An N.M.R. Investigation of the Mills-Nixon Effect
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The 4J coupling constant, previously established as a probe of bond order, was used to examine the bond orders in a series of ortho-bridged compounds: benzocyclopropene, 1,2-dihydrobenzocyclobutene, indan and tetralin.No evidence for sterically induced bond fixation (i.e. the Mills-Nixon effect) was found, but some evidence for electronic distortion in the corresponding benzylic ketones was observed.The experimental results are in accord with SCF/MO calculations.
- Collins, Michael J.,Gready, Jill E.,Sternhell, Sever,Tansey, Charles W.
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p. 1547 - 1557
(2007/10/02)
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- Kinetics and Mechanism of Oxidation of Fluoren-9-ol and Substituted Fluoren-9-ols by Bromamine-T
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The title reactions have been investigated in aq. acetic acid medium both in the presence and absence of perchloric acid.The reactions are first order each in and under both the conditions.There is unit dependence in perchloric acid.The effects of change in polarity of the solvent medium, added toluene-p-sulphonamide and sodium perchlorate have been studied.The reaction exhibits kinetic isotope effect (kH/kD = 2.2).Hammett ρ is found to be -2.8.Activation parameters have been evaluated.A mechanism consistent with rate data has been proposed.
- Gunasekaran, S.,Venkatasubramanian, N.
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p. 774 - 777
(2007/10/02)
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- INFLUENCE OF THE ANGULAR LINKAGE ON THE MESOMORPHIC PROPERTIES OF CHOLESTERYL ARYLBENZOATES.
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Some cholesteryl esters of arylbenzoic acids incorporating angular linkage such as -Co-, -O-, -S-, and -CH//2-, were prepared, and the transition temperatures and heats determined. The cholesteric-isotropic transition temperatures are likely to correlate with the angular correlation parameters of these carboxylic acid moieties. The mesomorphic phenomena are discussed in terms of the molecular structure and electronic effect of these linkages.
- Koden,Takenaka,Kusabayashi
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p. 137 - 150
(2007/10/02)
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- Rearrangement of arylhydrazones of aromatic and arylaliphatic carbonyl compounds to biphenyl derivatives. 3
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The behavior toward polyphosphoric acid of arylhydrazones of aromatic carbonyl compounds (anisaldehyde, substituted benzophenones, (4-methoxyphenyl)glyoxylic acid esters) and arylaliphatic ketones (4-methoxy- and 4-aminoacetophenone) is described.Biphenyl derivatives are formed through a sigmatropic rearrangement, which often occurs in competition with the expected Fischer indole synthesis and, in the case of the 4-amino-acetophenone 2,6-dimethylphenylhydrazone, with a completely new sigmatropic rearrangement.
- Fusco, R.,Sannicolo, F.
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- Electron acceptor monomers and polymers
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Disclosed are electron acceptor monomers of the formula: STR1 wherein R is STR2 or --H; R' is hydrogen or methyl; X and Y are independently selected from the group consisting of --NO2, halogen, cyano and --CF3 ; Z is oxygen or dicyanomethylene; and A and b can range from 0 to 3; with the proviso that at least one of R is STR3 and polymers prepared therefrom. These monomers and polymers are suitable for use in electrophotographic devices and methods.
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- Cyclic carbonyl compounds
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Certain fluorenone and anthraquinone compounds, each of which is 2-substituted by a carboxyl group or a salt, ester or optionally substituted amide thereof and each of which is optionally substituted in the 5,6-,7-or 8-position, by a second carboxyl group, salt, ester or optionally substituted amide thereof, the substitutent in the 5,6-7- or 8-position of the fluorenone compounds, also being selected from cyano, halogen, nitro, alkyl, alkoxy and acyl, are useful for the relief or prophylaxis of allergic conditions.
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- Cyclic carbonyl compounds
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Certain fluorenone and anthraquinone compounds, each of which is 2-substituted by a carboxyl group or a salt, ester or optionally substituted amide thereof and each of which is optionally substituted in the 5,6-,7- or 8- position, by a second carboxyl group, salt, ester or optionally substituted amide thereof, the substitutent in the 5,6-7- or 8- position of the fluorenone compounds, also being selected from cyano, halogen, nitro, alkyl, alkoxy and acyl, are useful for the relief or prophylaxis of allergic conditions.
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