- A bifunctional tungstate catalyst for chemical fixation of CO2 at atmospheric pressure
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No pressure: A simple monomeric tungstate, [WO4]2-, serves as a highly efficient homogeneous catalyst for various transformations of CO2 at atmospheric pressure. The tungsten-oxo moiety activates CO2 and the substrate simultaneously. The catalyst system is high yielding and applicable to a wide range of substrates such as amines (see scheme), 2-aminobenzonitriles, and propargylic alcohols. Copyright
- Kimura, Toshihiro,Kamata, Keigo,Mizuno, Noritaka
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- An easy one-step synthesis of imidazolin-2-ones from phthalic anhydrides and their antioxidant evaluation
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Treatment of phthalic anhydride derivatives with trimethylsilyl azide affords benzimidazolin-2-ones in 45-91% yield, which is the result of two consecutive Curtius reactions. Within the series obtained, 1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-one showed highest antioxidant activity.
- López, Héctor S.,Enciso, José E.,Ochoa-Terán, Adrián,Velazquez, Juan I.,Sarmiento, Juan I.
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- CdSnO3/SnD NPs as a Nanocatalyst for Carbonylation of o-Phenylenediamine with CO2
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In order to carbonize o-phenylenediamine with CO2, an effective approach was used with UV light irradiation by Sn(IV) doping DFNS (SnD) supported CdSnO3 as a catalyst (CdSnO3/SnD). In this catalyst, SnD with the ratios of Si/Sn in the range of 6 to 50 were obtained using the Direct Hydrothermal Synthesis (DHS), and the nanoparticles of CdSnO3 on the surfaces of SnD were reduced in situ. Scanning Electron Microscope (SEM), X-ray Diffraction (XRD), Fourier Transform Infrared Spectroscopy (FT-IR), X-ray Energy Dispersive Spectroscopy (EDS), and Transmission Electron Microscopy (TEM) were utilized for characterizing CdSnO3/SnD. It was found that CdSnO3/SnD nanostructures could be used for synthesizing o-phenylenediamines due to their effective and novel catalytic behavior through the reaction between o-phenylenediamines and CO2. Graphic Abstract: [Figure not available: see fulltext.]
- Liu, Can,Sadeghzadeh, Seyed Mohsen
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- Synthesis of benzimidazolones by immobilized gold nanoparticles on chitosan extracted from shrimp shells supported on fibrous phosphosilicate
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Here we demonstrate the synthesis of benzimidazolones from o-phenylenediamines and carbon dioxide in the presence of gold nanoparticles supported on a composite material based on microcrystalline chitosan from shrimp shells and fibrous phosphosilicate (CS-FPS/Au). The results showed that the gold nanoparticles were stable with the P, N and O atoms of CS-FPS. The morphology and structure of FPS leads to a higher catalytic activity. The CS-FPS/Au NPs were thoroughly characterized using TEM, FESEM, TGA, FTIR, and BET.
- Zahedifar, Mahboobeh,Es-Haghi, Ali,Zhiani, Rahele,Sadeghzadeh, Seyed Mohsen
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- 1,3-dimethyl benzimidazolones are potent, selective inhibitors of the brpf1 bromodomain
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The BRPF (bromodomain and PHD finger-containing) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. Here, we report the discovery, binding mode, and structure-activity relationship (SAR) of the firs
- Demont, Emmanuel H.,Bamborough, Paul,Chung, Chun-Wa,Craggs, Peter D.,Fallon, David,Gordon, Laurie J.,Grandi, Paola,Hobbs, Clare I.,Hussain, Jameed,Jones, Emma J.,Le Gall, Armelle,Michon, Anne-Marie,Mitchell, Darren J.,Prinjha, Rab K.,Roberts, Andy D.,Sheppard, Robert J.,Watson, Robert J.
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- IL4I1 INHIBITORS AND METHODS OF USE
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Described herein are compounds of Formula I or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as IL4I1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for IL4I1-related diseases.
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Page/Page column 128-129
(2021/11/13)
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- PrVO4/SnD NPs as a Nanocatalyst for Carbon Dioxide Fixation to Synthesis Benzimidazoles and 2-Oxazolidinones
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Recently CO2 stabilization has received a great deal of attention because of its probable applications as a rich C1 resource and the synthesis of several fine chemicals can be accomplished through this stabilization. In this study, Sn(IV) doping dendritic fibrous nanosilica (SnD) supported PrVO4 nanoparticles as a catalyst (PrVO4/SnD) was synthesized by a in-situ procedure. The SnD with the ratios of Si/Sn in a variety of 6 to 40 were acquired through direct hydrothermal synthesis (DHS), and PrVO4 NPs on the surfaces of SnD were reduced in-situ. X-Ray diffraction (XRD), Scanning electron microscope (SEM), Fourier transform infrared spectroscopy (FT-IR), transmission electron microscopy (TEM), and X-ray energy dispersive spectroscopy (EDS) were deployed for identifying the PrVO4/SnD. It is potentially a highly dynamic catalyst in the stabilization of CO2 for the production of 2-oxazolidinones and benzimidazoles. In addition, the catalyst is very easy to recycle and reuse without significant loss of active site Cu metal. Graphic Abstract: PrVO4/SnD NPs as a nanocatalyst for carbon dioxide fixation to synthesis benzimidazoles and 2-oxazolidinones. [Figure not available: see fulltext.]
- He, Zemin,Yu, Ping,Zhao, Yuzhen,Zhang, Huimin,Zhang, Yongming,Kang, Xiaoxi,Zhang, Haiquan,Sadeghzadeh, Seyed Mohsen
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p. 1623 - 1632
(2020/10/19)
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- SBA-15 Supported Dendritic ILs as a Green Catalysts for Synthesis of 2-Imidazolidinone from Ethylenediamine and Carbon Dioxide
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In this work, a simple and facile approach is conducted for preparing many new SBA-15 supported dendritic imidazolium ILs heterogeneous catalysts SBA-15/IL(1–3) having high ionic density from SBA-15. SBA-15/IL(3) as a green heterogeneous catalyst can be used for synthesis of 2-imidazolidinone from ethylenediamine and carbon dioxide and considering solvent-free condition. SBA-15/IL(3) showed to have the highest catalytic activity besides a positive dendritic influence on the yields of the synthesis of 2-imidazolidinone in the presence of CO2 is seen because of existing the high-density peripheral zwitterionic ionic liquid functional groups on the biobased SBA-15/IL(3) catalyst surfaces. Graphical Abstract: [Figure not available: see fulltext.]
- Liu, Jinghan,Ma, Jianjun,Miao, Penghua,Min, Qingwang,Qi, Meijuan,Shamsa, Farzaneh
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- BENZIMIDAZOLE DERIVATIVES AND THEIR USES
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The present invention provides compounds which inhibit the activity of TRPC6, pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof.
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Page/Page column 24-26
(2020/10/21)
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- Application of sea urchin-shaped cobalt-based photocatalyst in synthesis of benzoazacycle by converting CO2
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The invention relates to the technical field of photocatalysis, in particular to application of a sea urchin-shaped cobalt-based photocatalyst to synthesis of benzoazacycle by converting CO2. A complex is of a sea urchin-shaped microsphere structure, which is composed of an organic ligand L and cobalt nitrate hexahydrate and is formed by arranging a plurality of nano needle-shaped complex crystals. The main body of the organic ligand L is p-aminobenzoic acid; the application comprises the following steps: introducing CO2 into a solution containing o-phenylenediamine compounds, carrying out carbonylation reaction and cyclization with o-phenylenediamine compounds under the action of the urchin-shaped cobalt-based catalyst to generate the benzoazacycle compounds. The sea urchin-shaped microsphere structure cobalt-based catalyst formed by the obtained nano needle-shaped complex crystal has a very large specific surface area and high photocatalytic efficiency; when the photocatalyst is adopted to catalyze and activate CO2, the reaction for synthesizing the benzoazacycle by converting CO2 can be carried out at room temperature, so that the energy consumption is greatly reduced, and the cost is reduced.
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Paragraph 0029-0049
(2020/11/22)
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- Method for synthesizing benzothiazolone-based and 1,3-disubstituted urea-based derivatives through activation of CO2
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The present invention relates to a method for synthesizing benzothiazolone-based and 1,3-disubstituted urea-based derivatives through activation of CO2. According to the present invention, an inexpensive and easily-available sulfur-containing metal salt compound is first used as an activation catalyst for CO2, and a reaction raw material and CO2 are converted into a corresponding target compound at a low reaction temperature under a low CO2 pressure; and the method has high atomic economy, can reduce the generation of by-products, meets the standards of environmental friendliness and environmentally friendly chemistry, and is the effective way capable of completely utilizing CO2 as the renewable resource, developing new energy and achieving the beneficial cycle of carbon in nature.
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Paragraph 0054; 0055; 0056; 0059; 0060
(2018/09/12)
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- SMALL MOLECULE REGULATORS OF STEROID RECEPTOR COACTIVATORS AND METHODS OF USE THEREOF
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Small molecule regulators of steroid receptor coactivator (SRC) family proteins are provided, as well as methods for their use in treating or preventing SRC-related diseases. The SRC-related diseases can include cancer, metabolic disorders, human immunodeficiency virus, neurodegenerative disorders, and/or inflammatory diseases. Also provided are methods for regulating SRC family proteins in a cell.
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Paragraph 0277; 0278
(2017/10/27)
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- 1,3-DIMETHYLBENZIMIDAZOLONE DERIVATIVE AS AN INHIBITOR OF THE BRPF1 BROMODOMAIN
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A novel benzoimidazolyl compound, pharmaceutical compositions containing such a compound and its use in therapy.
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Page/Page column 24
(2016/06/06)
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- GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain
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The BRPF (Bromodomain and PHD Finger-containing) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. A selective benzimidazolone BRPF1 inhibitor showing micromolar activity in a cellular target engag
- Bamborough, Paul,Barnett, Heather A.,Becher, Isabelle,Bird, Mark J.,Chung, Chun-Wa,Craggs, Peter D.,Demont, Emmanuel H.,Diallo, Hawa,Fallon, David J.,Gordon, Laurie J.,Grandi, Paola,Hobbs, Clare I.,Hooper-Greenhill, Edward,Jones, Emma J.,Law, Robert P.,Le Gall, Armelle,Lugo, David,Michon, Anne-Marie,Mitchell, Darren J.,Prinjha, Rab K.,Sheppard, Robert J.,Watson, Allan J. B.,Watson, Robert J.
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supporting information
p. 552 - 557
(2016/07/06)
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- Azole-Anion-Based Aprotic Ionic Liquids: Functional Solvents for Atmospheric CO2 Transformation into Various Heterocyclic Compounds
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The chemical transformation of atmospheric CO2 is of great significance yet still poses a great challenge. Herein, azole-anion-based aprotic ionic liquids (ILs) were synthesized by the deprotonation of weak proton donors (e.g., 2-methylimidazole, 4-methylimidazole, and 2,4-dimethylimidazole) with tetrabutylphosphonium hydroxide, [Bu4P][OH]. We found that these ILs, such as [Bu4P][2-MIm], could activate atmospheric CO2 through the formation of carbamates. The resultant carbamate intermediates could further react with various types of substrate, including propargylic alcohols, 2-aminobenzonitriles, ortho-phenylenediamines, and 2-aminothiophenol, thereby producing α-alkylidene cyclic carbonates, quinazoline-2,4(1 H,3 H)-diones, benzimidazolones, and benzothiazoline, respectively, in moderate-to-good yields. Thus, we have achieved the transformation of CO2 at atmospheric pressure, and we expect this method to open up new routes for the synthesis of various oxygen-containing heterocyclic compounds under metal-free conditions.
- Zhao, Yanfei,Wu, Yunyan,Yuan, Guangfeng,Hao, Leiduan,Gao, Xiang,Yang, Zhenzhen,Yu, Bo,Zhang, Hongye,Liu, Zhimin
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p. 2735 - 2740
(2016/10/11)
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- Facile Synthesis of Benzo[ d ]azol-2(3 H)-ones Using 2-Phenoxycarbonyl-4,5-dichloropyridazin-3(2 H)-one as Green CO Source
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Developing eco-friendly, stable, and easy-to-handle acyl sources is of great importance in synthetic and green chemistry. This study describes the synthesis of benzo[d]azol-2(3H)-ones such as benzo[d]thiazol-2(3H)-ones, benzo[d]oxazol-2(3H)-ones, and benzo[d]imidazol-2(3H)-ones using 2-phenoxycarbonyl-4,5-dichloropyridazin-3(2H)-one in one pot. The reaction reported is carried out under neutral or acidic conditions in the presence of zinc or sodium bicarbonate to give the corresponding heterocycles in good to excellent yields. The reaction uses a solid stable carbonyl source that is a recyclable functional-group carrier, pyridazin-3(2H)-one.
- Ryu, Ki Eun,Kim, Bo Ram,Sung, Gi Hyeon,Yoon, Hyo Jae,Yoon, Yong-Jin
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supporting information
p. 1985 - 1990
(2015/09/01)
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- Scope of chemical fixation of carbon dioxide catalyzed by a bifunctional monomeric tungstate
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The tungsten-oxo moiety in a simple monomeric tungstate, TBA 2[WO4] (I, TBA = tetra-n-butylammonium), showed bifunctional activation of both CO2 and 1,2-phenylenediamine (1a). It was confirmed by 1H, 13C, and 183W NMR spectroscopies that adducts I-1a and I-(CO2)n (n = 1 and 2) were formed by the reactions of I with 1a and CO2, respectively. These adducts played important roles in formation of the corresponding carbamic acid intermediates. The present bifunctionality could be applied to chemical fixation of CO2 even at atmospheric pressure with various kinds of structurally diverse aryl diamines, primary monoamines, propargylic alcohols, and propargylic amines into cyclic urea derivatives, 1,3-disubstituted urea derivatives, cyclic carbonates, and cyclic carbamates, respectively.
- Kamata, Keigo,Kimura, Toshihiro,Sunaba, Hanako,Mizuno, Noritaka
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p. 160 - 166
(2014/03/21)
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- DBU-based ionic-liquid-catalyzed carbonylation of o-phenylenediamines with CO2 to 2-benzimidazolones under solvent-free conditions
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Herein, a new route was presented to synthesize 2-benzimidazolones via the carbonylation of o-phenylenediamines with CO2 catalyzed by 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU)-based ionic liquids under solvent-free conditions. DBU acetate ([DBUH][OAc]) displayed high efficiency for catalyzing the reactions of CO2 with o-phenylenediamines, and a series of benzimidazolones were obtained in high yields. It was demonstrated that [DBUH][OAc] could serve as a bifunctional catalyst for these reactions with the cation activating CO2 and the anion activating o-phenylenediamines. This protocol provides an effective and environmentally friendly alternative route for production of benzimidazolones, and extends the chemical utilization of CO2 in organic synthesis as well.
- Yu, Bo,Zhang, Hongye,Zhao, Yanfei,Chen, Sha,Xu, Jilei,Hao, Leiduan,Liu, Zhimin
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p. 2076 - 2082
(2013/09/24)
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- CHEMICAL COMPOUNDS
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There is provided pyrimidinyl compounds of Formula (I), wherein: R2 is or pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
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(2012/01/03)
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- BENZIMIDAZOLES WITH A HETERO SPIRO-DECANE RESIDUE AS NPY-Y5 ANTAGONISTS
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The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salts, solvates, stereoisomers thereof, formula (I), R1 may be C1-C4 alkyl, aryl or heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; R2 may be halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano, nitro; or aryl, heteroaryl or heterocycle, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; or R2 may correspond to -0-R3; R3 is a 6-membered aromatic carbocyclic ring which may contain 1 or 2 nitrogen X is carbon or oxygen; Z is carbon or nitrogen; G is a fused 6-membered aromatic carbocyclic ring which may contain 1 or 2 nitrogen; m may be 0 or an integer ranging from 1 to 4; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY- Y5 receptor antagonists.
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(2008/12/08)
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- Design of potent, orally available antagonists of the transient receptor potential vanilloid 1. Structure-activity relationships of 2-piperazin-1-yl-1H- benzimidazoles
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The vanilloid receptor-1 (VR1 or TRPV1) is a membrane-bound, nonselective cation channel that is predominantly expressed by peripheral neurons sensing painful stimuli. TRPV1 antagonists produce antihyperalgesic effects in animal models of inflammatory and neuropathic pain. Herein, we describe the synthesis and the structure-activity relationships of a series of 2-(4-pyridin-2- ylpiperazin-1-yl)-1H-benzo-[d]imidazoles as novel TRPV1 antagonists. Compound 46ad was among the most potent analogues in this series. This compound was orally bioavailable in rats and was efficacious in blocking capsaicin-induced flinch in rats in a dose-dependent manner. Compound 46ad also reversed thermal hyperalgesia in a model of inflammatory pain, which was induced by complete Freund's adjuvant (CFA).
- Ognyanov, Vassil I.,Balan, Chenera,Bannon, Anthony W.,Bo, Yunxin,Dominguez, Celia,Fotsch, Christopher,Gore, Vijay K.,Klionsky, Lana,Ma, Vu V.,Qian, Yi-Xin,Tamir, Rami,Wang, Xianghong,Xi, Ning,Xu, Shimin,Zhu, Dawn,Gavva, Narender R.,Treanor, James J. S.,Norman, Mark H.
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p. 3719 - 3742
(2007/10/03)
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- BENZIMIDAZOLE DERIVATIVES AND THEIR USE AS VANILLOID RECEPTOR LIGANDS
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Compounds of formula (I) are useful in the treatment of vanilloid-receptor-meditated diseases, such as inflammatory or neuropathic pain and diseases involving sensory nerve function such as asthma, rheumatoid arthritis, osteoarthritis, inflammatory bowel disorders, urinary incontinence, migraine and psoriasis.
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- PROLINE DERIVATIVES AND USE THEREOF AS DRUGS
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The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products. The present inventors have found that derivatives having a substituent introduced into the γ-position of proline represented by the formula (I) wherein each symbol is as defined in the specification, have a potent DPP-IV inhibitory activity, and completed the present invention by increasing the stability.
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- SUBSTITUTED ARYL AND CYCLOALKYL IMIDAZOLONES; A NEW CLASS OF GABA BRAIN RECEPTOR LIGANDS
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Disclosed are compounds of the formula: STR1 wherein: T is NH, O, or S;X is hydrogen, hydroxyl, lower alkyl, or an optionally substituted amide;the W ring is an optionally substituted aryl or heteroaryl group; and STR2 represents an optionally substituted benzo group or an optionally substituted 5, 6, 7, or 8 membered ring.These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.
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