- Cu(OAc)2-Mediated benzimidazole-directed C-H cyanation using 2-(4-methylpiperazin-1-yl)acetonitrile as the cyano source
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A new protocol for the Cu(OAc)2-mediated cyanation of arenes using benzimidazole as the directing group with 2-(4-methylpiperazin-1-yl)acetonitrile as the cyano source was developed. A series of cyano derivatives were facilely and conveniently obtained in moderate to good yields by using this method. The C-H activation catalytic system was originally applied to the C(sp2)-H cyanation of the aryl/heteroaryl to synthesize 2-(1H-benzo[d]imidazol-2-yl)aryl nitriles. There were 19 new compounds in the synthesized 20 cyanide products. In this reaction, 2-(4-methylpiperazin-1-yl)acetonitrile as the cyano source was originally employed in the C(sp2)-H cyanation of the arenes. In addition, a fluorescent material 5a was obtained by derivative reactions of the obtained cyanide product 3.
- Zhang, Tianyou,Qiao, Jingyi,Song, He,Xu, Feng,Liu, Xiaochong,Xu, Chunzhao,Ma, Junjie,Liu, Hao,Sun, Zhizhong,Chu, Wenyi
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Read Online
- Synthesis and characterization of bis[2-(1H-Benzimidazol-2-yl)benzoato] nickel(II), and its use for preparation of dimethyl carbonate from methanol and CO2
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A new complex, bis[2-(1H-benzimidazol-2-yl)benzoato]nickel(II) (NiL 2), has been synthesized and characterized. It was used as catalyst for synthesis of dimethyl carbonate (DMC) from methanol and CO2 in the presence of dicyclohexyl c
- Shi, Yanning,Jin, Xilang,Hu, Yechen,Wang, Shuli,Li, Jianli,Shi, Zhen
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Read Online
- Wavelength dependent photoextrusion and tandem photo-extrusion reactions of ninhydrin bis-acetals for the synthesis of 8-ring lactones, benzocyclobutenes and orthoanhydrides
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Ninhydrin bis-acetals give access to 8-ring lactones, benzocyclo-butenes and spirocyclic orthoanhydrides through photoextrusion and tandem photoextrusion reactions. Syntheses of fimbricalyxlactone B, isoshihunine and numerous biologically-relevant heteroc
- George, Michael W.,Hanson-Heine, Magnus W. D.,Harrowven, David C.,Kayal, Surajit,Light, Mark E.,Raimbach, William A. T.,Sun, Wei,Sun, Xue-Zhong
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p. 1546 - 1549
(2022/02/14)
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- Composition based on benzimidazole carboxylic acid compound and application thereof
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The invention belongs to the field of medicine and pharmacology, and particularly relates to a pharmaceutical composition taking benzimidazole carboxylic acid and pharmaceutically acceptable salt thereof as active ingredients. The pharmaceutical composition taking the benzimidazole carboxylic acid and pharmaceutically acceptable salt thereof as main active ingredients is used for preventing and/ortreating respiratory tract reaction and nasal congestion caused by allergic reaction, nasal congestion caused by other reasons and other symptoms, and can realize immediate and/or lasting alleviationof congestion. The invention also provides a method of treating and/or alleviating and/or preventing nasal congestion in a patient, the method comprising administering to a patient in need thereof aneffective amount of the pharmaceutical composition of the benzimidazole carboxylic acid or a pharmaceutically acceptable salt thereof.
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Paragraph 0058; 0064; 0075-0077
(2020/10/14)
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- SYNTHESIS METHOD OF IMIDAZOLES
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PROBLEM TO BE SOLVED: To provide benzimidazoles with small number of processes at high selectivity and high purity. SOLUTION: A synthesis method of benzimidazoles synthesizes at least one of an imidazole derivative and a carboxy imidazole derivative by reacting a diamine derivative and at least one of a dicarboxylic acid derivative and a dicarboxylic acid anhydride derivative in subcritical water or in supercritical water. For example, in subcritical water or in supercritical water, by reacting o-phenylene diamine and at least one of phthalic acid and phthalic anhydride, 2-phenylbenzimidazole and 2-o-benzimidazole benzoate are synthesized. SELECTED DRAWING: None COPYRIGHT: (C)2019,JPOandINPIT
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Paragraph 0106; 0107
(2019/05/15)
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- 2-benzimidazolyl benzoic acid copper complex with anti-fungal activity and preparation method
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The invention discloses a 2-benzimidazolyl benzoic acid copper complex with anti-fungal activity and a preparation method. The complex is prepared by the following steps: taking 2-benzimidazolyl benzoic acid and Cu(NO3)2.3H2O to react in a mixed solvent o
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Paragraph 0024; 0025; 0026; 0027
(2017/09/01)
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- Substituted 2-formylbenzoic acids in the synthesis of 11H-isoindolo[2,1-a] benzimidazol-11-ones, 5H-isoindolo[2,1-a][3,1]benzoxazine-5,11(6aH)-diones, and 6,6a-dihydroisoindolo-[2,1-a]quinazoline-5,11-diones
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Optimal conditions were developed for the synthesis of 11H-isoindolo[2,1-a] benzimidazol-11-one, 5H-isoindolo[2,1-a][3,1]benzoxazine-5,11(6aH)-dione, and 6,6a-dihydroisoindolo[2,1-a]quinazoline-5,11-dione derivatives in the reaction of substituted 2-formylbenzoic acids with o-phenylenediamine, anthranilic acid, and anthranilamide, respectively. The bifolded structure of 6,6a- dihydroisoindolo-[1,2-a]quinazoline-5,11-dione was verified and investigated.
- Gromachevskaya,Fin'Ko,Butin,Pushkareva,Strelkov,Isakova,Krapivin
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p. 1331 - 1344
(2014/01/17)
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- An efficiently cobalt-catalyzed carbonylative approach to phenylacetic acid derivatives
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A highly efficient cobalt-catalyzed carbonylative approach to phenylacetic acid derivatives under one atmosphere pressure is reported. This methodology represents a useful extension of benzimidazole used as ligand in metal catalysis, and the catalytic mechanism has been proved by computer simulation. Notably, this new cobalt precatalyst, which promotes the carbonylation reaction dramatically and has already been used for scale-up experiment of phenylacetic acid derivatives.
- She, Meng-Yao,Xiao, Da-Wei,Yin, Bing,Yang, Zheng,Liu, Ping,Li, Jian-Li,Shi, Zhen
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p. 7264 - 7268
(2013/08/23)
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- A new laccase-catalyzed domino process and its application to the efficient synthesis of 2-aryl-1H-benzimidazoles
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The laccase-catalyzed domino reaction of o-phenylenediamine and benzaldehydes with aerial oxygen as the oxidant exclusively yields 2-aryl-1H-benzimidazoles in good to very good yields. It is easy to perform under very mild reaction conditions.
- Leutbecher, Heiko,Constantin, Mihaela-Anca,Mika, Sabine,Conrad, Jürgen,Beifuss, Uwe
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experimental part
p. 605 - 608
(2011/03/18)
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- Green synthesis of polycyclic benzimidazole derivatives and organic semiconductors
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Polycyclic benzimidazole derivatives, an important class of compounds in organic electronics and photovoltaics, were prepared using a solvent-free "green" process based on heating carboxylic acid anhydrides and arylene diamines in the presence of zinc acetate in the solid state. Products were isolated and purified directly by train sublimation of the crude reaction mixtures. The reaction conditions were optimized using various carboxylic acid anhydrides. Optical and electrochemical properties of these materials are also described.
- Mamada, Masashi,Perez-Bolivar, Cesar,Anzenbacher, Pavel
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scheme or table
p. 4882 - 4885
(2011/12/05)
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- Synthesis and QSAR evaluation of 2-(substituted phenyl)-1H-benzimidazoles and [2-(substituted phenyl)-benzimidazol-1-yl]-pyridin-3-yl-methanones
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A series of 2-(substituted phenyl)-1H-benzimidazole (1-10) and [2-(substituted phenyl)-benzimidazol-1-yl]-pyridin-3-yl-methanone (11-19) derivatives were synthesized and tested in vitro for their antimicrobial activity. The results of QSAR investigation indicated the importance of molecular descriptors, dipole moment (μ), log of octanol water partition coefficient (log P) and second order molecular connectivity index (2χ) in describing the antimicrobial activity of the synthesized compounds.
- Sharma, Deepika,Narasimhan, Balasubramanian,Kumar, Pradeep,Jalbout, Abraham
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experimental part
p. 1119 - 1127
(2009/10/02)
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- Benzimidazol-2-yl or benzimidazol-2-ylthiomethyl benzoylguanidines as novel Na+/H+ exchanger inhibitors, synthesis and protection against ischemic-reperfusion injury
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A novel series of benzimidazol-2-yl or benzimidazol-2-ylthiomethyl benzoylguanidines were designed and synthesized as Na+/H+exchanger inhibitors. Most of them were found to inhibit NHE1-mediated platelet swelling in a concentration-dependent manner, and to have significant cardioprotective effect against myocardial ischemic-reperfusion injury, among which compounds 10a and 34 were more potent than cariporide in both in vivo and in vitro tests.
- Zhang, Rui,Lei, Lin,Xu, Yun-Gen,Hua, Wei-Yi,Gong, Guo-Qing
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p. 2430 - 2433
(2008/04/18)
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- Synthesis and antiviral activities of N-substituted-2-substituted- benzimidazole derivatives
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Two series of N-substituted-2-substituted benzimidazole derivatives, viz. 1-benzyl-2-substituted benzimidazole 8-14 and 1-(p-chlorophenyl)-2-substituted benzimidazole 15-21 have been synthesized and tested for their antiviral activities. These compounds have been screened for Tobacco mosaic viruses and Sunhemp rosette viruses and show significant activities.
- Tewari, Ashish Kumar,Mishra, Anil
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p. 489 - 493
(2007/10/03)
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- A new kinetic model for the acid-catalysed reactions of N-(2-aminophenyl)phthalamic acid in aqueous media
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The acid-catalysed breakdown of N-(2-aminophenyl)phthalamic acid has been studied in dilute aqueous acids in the pH range 0-6. The dominant reaction is the formation of N-(2-aminophenyl)phthalimide (between ~80 and ~100% yields in the pH range studied) and its subsequent rearrangement to 2-(2-carboxyphenyl)benzimidazole, occurring as consecutive pseudo-first-order processes. Anomalously, only a minor hydrolysis reaction is observed. A kinetic model for these processes has been constructed and rate constants and activation parameters evaluated. Mechanisms involving pre-equilibria to form the kinetically significant species have been proposed for the consecutive processes. The approach has been adapted to account for the observed kinetics of acid catalysed formation of benzimidazoles from o-aminoanilides.
- Perry, Christopher J.
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p. 977 - 982
(2007/10/03)
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- Tunneling proton transfer in the general basic hydrolysis of the methyl ester of methyl ester of imidazolylbenzoic acid
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We have studied the temperature dependence of the rate constant for the intramolecular general basic hydrolysis of the methyl ester of 2-(2'-imidazolyl)benzoic acid in water and in heavy water (D2O).The kinetic isotope effect of the solvent at 40-60 deg C was found to be 3.4, with activation energies of EaH = 55.8 +/- 0.8 and EaD = 54.2 +/- 1.2 kJ mol-1 respectively.We conclude that the motion of the proton during the elementary act of the rate-limiting step in the nucleophilic attack has a mainly tunneling character.
- Goguadze, N. G.,Khoshtariya, D. E.,Krishtalik, L. I.,Yatsimirskii, A. K.,Deiko, S. A.,Neverov, A. A.
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p. 135 - 136
(2007/10/02)
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