- Novel preparation method of antihypertensive drug telmisartan intermediate
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The invention relates to an electric reduction preparation method of aminobenzoic acid represented by formula I and ester thereof. The preparation reaction of the method is shown in the description; and in the reaction formula, R is selected from hydrogen, a methyl group, an ethyl group, a benzyl group, a C3 or C4 straight-chain alkyl or branched-chain alkyl group, -NO2 is selected from 4-NO2 or 5-NO2, and Y is selected from H or 4-NHCOC3H7-n. The electroreduction preparation method of aminobenzoic acid and ester I thereof is characterized in that in a separated electrolytic cell, an acidic solution of nthe itrobenzoic acid and ester III thereof is taken as a catholyte; the voltage of a cathode working electrode relative to a reference electrode is 1.00-2.50 V; and an anolyte is an acidicsolution, the current density is 25.0-250.0 mA/cm, and the electrolysis temperature is 15-90 DEG C.
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Paragraph 0066-0069
(2021/06/26)
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- O-nitrophenyl ethanol derivative as well as preparation method and application thereof
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The invention discloses an o-nitrophenethyl alcohol derivative and a preparation method and application thereof, the structural formula of the o-nitrophenethyl alcohol derivative is shown in the specification, and R is C1-C18 alkyl. The invention provides
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Paragraph 0045-0049
(2021/04/17)
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- N-transfer reagent and method for preparing the same and its application
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Provided are a novel N-transfer reagent and a method for preparing the same and its application. The N-transfer reagent is represented by the following Formula (I): The various novel N-transfer reagents of the present invention can be quickly prepared by employing different nitrobenzene precursors. The N-transfer reagents can directly convert a variety of amino compounds into diazo compounds under mild conditions. Particularly, the N-transfer reagents can facilitate the synthesis of the diazo compounds. The application of synthesizing diazo compounds of the present invention can greatly decrease the difficulty in operation, increase the safety during experiments, reduce the cost of production and the environmental pollution, and enhance the industrial value of diazo compounds.
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Page/Page column 14-15
(2021/06/25)
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- Aromatic acyl hydrazone derivative and application thereof as NA inhibitor
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The invention relates to an aromatic acyl hydrazone derivative as shown in a structural formula I, pharmaceutically acceptable salt and a pharmaceutical composition thereof, and application of the aromatic acyl hydrazone derivative and the pharmaceutically acceptable salt and the pharmaceutical composition in preparation of an influenza virus neuraminidase inhibitor, wherein R is one of trifluoromethyl, nitryl, 3-methyl-4-nitryl, 3-hydroxyl-4-nitryl, 3-nitryl-4-hydroxyl, hydroxyl, dihydroxyl, dinitryl, 3-methoxy-4-hydroxyl or trihydroxyl; Y is selected from hydroxyl, dihydroxyl, 2-hydroxyl-3-methoxy, 2-hydroxyl-4-methoxy,2-hydroxyl-5-methoxy,2-hydroxyl-6-methoxy,3-hydroxyl-2-methoxy,3-hydroxyl-4-methoxy,3-hydroxyl-5-methoxy,3-hydroxyl-6-methoxy,4-hydroxyl-2-methoxy,4-hydroxyl-3-methoxy,4-hydroxyl-3,5-dimethoxy, trihydroxyl, 4-hydroxyl-3-ethoxy, or 4-hydroxyl-3,5-dimethoxy; w is selected from CH or N; and z is selected from CH or N.
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Paragraph 0039-0043; 0110-0114
(2020/12/30)
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- Antifungal activity of cinnamic acid and benzoic acid esters against Candida albicans strains
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Candida albicans is an important opportunistic fungal pathogen capable of provoking infection in humans. In the present study, we evaluated the antifungal effect of 23 ester derivatives of the cinnamic and benzoic acids against 3 C. albicans strains (ATCC-76645, LM-106 and LM-23), as well as discuss their Structure–Activity Relationship (SAR). The antifungal assay results revealed that the screened compounds exhibited different levels of activity depending on structural variation. Among the ester analogues, methyl caffeate (5) and methyl 2-nitrocinnamate (10) were the analogues that presented the best antifungal effect against all C. albicans strains, presenting the same MIC values (MIC?=?128?μg/mL), followed by methyl biphenyl-2-carboxylate (21) (MIC?=?128, 128 and 256?μg/mL for C. albicans LM-106, LM-23, and ATCC-76645, respectively). Our results suggest that certain molecular characteristics are important for the antifungal action.
- Lima, Tamires C.,Ferreira, Alana R.,Silva, Daniele F.,Lima, Edeltrudes O.,de Sousa, Dami?o P.
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p. 572 - 575
(2017/09/30)
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- C1-Phostphonate Analogue of UDP-GlcNAc for Inhibition of O-GlcNAc Transferase
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A novel C1-phosphate analogue of uridine-5′-diphosphate (UDP)-GlcNAc as an effective OGT (O-linked N-acetylglucosamine (O-GlcNAc) transferase) inhibitor, and a preparation method for the same provides a compound having an OGT inhibitory effect that can be
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Paragraph 0030; 0031
(2017/02/24)
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- Preparation method of highly selective 3-methyl-2-nitrobenzoic acid
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The invention discloses a preparation method of 3-methyl-2-nitrobenzoic acid. 3-methylbenzoic acid alkyl ester is used as raw material in nitrification, two-grade selectivity and high yield are realized, and the amount of waste acid was reduced. In nitrification product, only 3-methyl 2-nitrobenzoic acid alkyl ester and 3-methyl-4-nitrobenzoic acid alkyl ester are hydrolyzed after separation to obtain 3-methyl 2-Nitrobenzoic acid and 3-methyl-4-nitrobenzoic acid. The process is simple, and suitable for industrial production.
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- Conversion of alcohols to alkyl esters and carboxylic acids using heterogeneous palladium-based catalysts
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Disclosed are methods for synthesizing an ester or a carboxylic acid from an organic alcohol. To form the ester one reacts, in the presence of oxygen gas, the alcohol with methanol or ethanol. This reaction occurs in the presence of a catalyst comprising palladium and a co-catalyst comprising bismuth, tellurium, lead, cerium, titanium, zinc and/or niobium (most preferably at least bismuth and tellurium). Alternatively that catalyst can be used to generate an acid from that alcohol, when water is also added to the reaction mix.
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- Synthesis of a benzene-containing C1-phosphonate analogue of UDP-GlcNAc for the inhibition of O-GlcNAc transferase
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I report here the design, synthesis, and biological evaluation of a new C1-phosphonate analogue of UDP-GlcNAc as a potential inhibitor of OGT, an enzyme responsible for O-GlcNAc modification. The analogue was designed to mimic the transition state of the
- Im, Jungkyun
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- Synthesis method for 3-formyl-4-methyl nitrobenzoate
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The invention relates to a synthesis method for a compound, in particular to a synthesis method for 3-formyl-4-methyl nitrobenzoate.According to synthesis method, a simple and cheap preparation method for 3-formyl-4-methyl nitrobenzoate is supplied, the reaction conditions in the preparation process are mild, and the yield is high.
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Paragraph 0003; 0006
(2016/10/27)
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- Preparation method of 3-methoxy-2-nitrobenzoate
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The invention discloses a preparation method of 3-methyl-2-nitrobenzoate. The preparation method has the advantages that firstly 3-methyl benzoate is taken as a starting material, nitrification, reduced-pressure concentration, washing with ice water, filt
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Paragraph 0016
(2017/05/16)
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- One-dimensional channels encapsulated in supramolecular networks constructed of zinc(II), manganese(II), or nickel(II) atoms with 3-(Carboxymethyl)-2, 7-dimethyl-3H-benzo[d]imidazole-5-carboxylic Acid
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Four complexes with supramolecular architectures, namely, MZCA·3H2O (1), [Zn(H2O)6] 2+·[MZCA]2·[H2O]6 (2), [Mn(MZCA)2(H2O)4]·2H2O (3), and [Ni(MZCA)2(H2O)4]·2H2O (4) [MZCA = 3-(carboxymethyl)-2, 7-dimethyl-3H-benzo[d]imidazole-5-carboxylic acid], were synthesized and characterized by elemental analysis, IR spectroscopy, and single-crystal X-ray diffraction. Complexes 1 and 2 display a remarkable 3D network with 1D hydrophilic channels. Complexes 3 and 4 are isostructural and exhibit a 3D structure encapsulating 1D 24-membered ring microporous channels. The UV/Vis and fluorescent spectra were measured to characterize complexes 1-4. The thermal stability of complexes 2-4 were also examined.
- Zhao, Mingxia,Xiong, Liqin,Li, Shilei,Chang, Jin,Ning, Hongyu,Qi, Chuanmin
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p. 159 - 167
(2014/01/23)
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- One-pot synthesis of novel 3,5-disubstituted-1,2,4-oxadiazoles from indazole carboxylic acid esters and amidoximes
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An efficient and high-yielding one-pot synthesis of 3,5-disubstituted-1,2, 4-oxadiazoles from indazole carboxylic acid methyl esters and amidoximes is described. In this study a series of novel 3,5-disubstituted-1,2,4-oxadiazoles (3a-d), (4a-d), (5a-d), (6a-d), (7a-d) were synthesized using amidoximes 2a-d and indazole carboxylic acid esters (3-6).
- Swamy, Udutha Kumara,Mohan, H. Rama,Prasad, U. Viplava,Suresh,Kumar, T. Laxmi
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p. 1921 - 1930
(2014/06/09)
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- Copper-catalyzed decarboxylative methylation of aromatic carboxylic acids with PhI(OAc)2
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The copper-catalyzed decarboxylative methylation of aromatic carboxylic acids was developed by using PhI(OAc)2 to provide a new strategy for the methylation of aryl acids through the decarboxylation of alkyl acids. The mechanism and the roles of each reactant in the reaction were investigated extensively. Copyright
- Jiang, Yuyu,Pan, Shulei,Zhang, Yanghui,Yu, Jingxun,Liu, Hongqiang
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supporting information
p. 2027 - 2031
(2014/04/17)
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- Structure-activity relationship study on benzoic acid part of diphenylamine-based retinoids
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Based on structure-activity relationship studies of the benzoic acid part of diphenylamine-based retinoids, the potent RXR agonist 4 was derivatized to obtain retinoid agonists, synergists, and an antagonist. Cinnamic acid derivatives 5 and phenylpropionic acid derivatives 6 showed retinoid agonistic and synergistic activities, respectively. The difference of the activities is considered to be due to differences in the flexibility of the carboxylic acid-containing substituent on the diphenylamine skeleton. Compound 7, bearing a methyl group at the meta position to the carboxyl group, was an antagonist, dose-dependently inhibiting HL-60 cell differentiation induced by 3.3 × 10-10 M Am80.
- Ohta, Kiminori,Kawachi, Emiko,Shudo, Koichi,Kagechika, Hiroyuki
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-
- Aerobic oxidation of diverse primary alcohols to methyl esters with a readily accessible heterogeneous Pd/Bi/Te catalyst
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Efficient aerobic oxidative methyl esterification of primary alcohols has been achieved with a heterogeneous catalyst consisting of 1 mol % Pd/charcoal (5 wt %) in combination with bismuth(III) nitrate and tellurium metal. The Bi and Te additives significantly increase the reaction rate, selectivity, and overall product yields. This readily accessible catalyst system exhibits a broad substrate scope and is effective with both activated (benzylic) and unactivated (aliphatic) alcohols bearing diverse functional groups.
- Powell, Adam B.,Stahl, Shannon S.
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supporting information
p. 5072 - 5075
(2013/10/22)
-
- HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK
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Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
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Page/Page column 33
(2012/11/08)
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- Hysteretic carbon dioxide sorption in a novel copper(ii)-indazole- carboxylate porous coordination polymer
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The synthesis, structural and gas sorption studies of a porous Cu(ii) coordination polymer featuring 1H-indazole-5-carboxylic acid (H2L) are presented. [Cu(HL)2] is a thermally and hydrolytically robust 4-connected 3D coordination polymer of NbO topology and is replete with 1D channels that permit selective and hysteretic sorption of CO2. The Royal Society of Chemistry 2012.
- Hawes, Chris S.,Babarao, Ravichandar,Hill, Matthew R.,White, Keith F.,Abrahams, Brendan F.,Kruger, Paul E.
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supporting information
p. 11558 - 11560
(2013/01/15)
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- Pyrrolidinobenzoic acid inhibitors of influenza virus neuraminidase: The hydrophobic side chain influences type A subtype selectivity
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Neuraminidase (NA) plays a critical role in the life cycle of influenza virus and is a target for new therapeutic agents. A series of influenza neuraminidase inhibitors with the pyrrolidinobenzoic acid scaffold containing lipophilic side chains at the C3 position have been synthesized and evaluated for influenza neuraminidase inhibitory activity. The size and geometry of the C3 side chains have been modified in order to investigate structure-activity relationships. The results indicated that size and geometry of the C3-side chain are important for selectivity of inhibition against N1 versus N2 NA, important type A influenza variants that infect man, including the highly lethal avian influenza.
- Li, Yanwu,Silamkoti, Arundutt,Kolavi, Gundurao,Mou, Liyuan,Gulati, Shelly,Air, Gillian M.,Brouillette, Wayne J.
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experimental part
p. 4582 - 4589
(2012/09/05)
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- Chromo-fluorogenic detection of nerve-agent mimics using triggered cyclization reactions in push-pull dyes
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A family of azo and stilbene derivatives (1-9) are synthesized, and their chromo-fluorogenic behavior in the presence of nerve-agent simulants, diethylchlorophosphate (DCP), diisopropylfluorophosphate (DFP), and diethylcyanophosphate (DCNP) in acetonitrile and mixed solution of water/acetonitrile (3:1 v/v) buffered at pH 5.6 with MES, is investigated. The prepared compounds contain 2-(2-N,N-dimethylaminophenyl) ethanol or 2-[(2-N,N-dimethylamino)phenoxy]ethanol reactive groups, which are part of the conjugated π-system of the dyes and are able to give acylation reactions with phosphonate substrates followed by a rapid intramolecular N-alkylation. The nerve-agent mimic-triggered cyclization reaction transforms a dimethylamino group into a quaternary ammonium, inducing a change of the electronic properties of the delocalized systems that results in a hypsochromic shift of the absorption band of the dyes. Similar reactivity studies are also carried out with other "non-toxic" organophosphorus compounds, but no changes in the UV/Vis spectra were observed. The emission behaviour of the reagents in acetonitrile and water-acetonitrile 3:1 v/v mixtures is also studied in the presence of nerve-agent simulants and other organophosphorous derivatives. The reactivity between 1-9 and DCP, DCNP, or DFP in buffered water-acetonitrile 3:1 v/v solutions under pseudo first-order kinetic conditions, using an excess of the corresponding simulant, are studied in order to determine the rate constants (k) and the half-life times (t1/2=ln2/k) for the reaction. The detection limits in water/acetonitrile 3:1 v/v are also determined for 1-9 and DCP, DCNP, and DFP. Finally, the chromogenic detection of nerve agent simulants both in solution and in gas phase are tested using silica gel containing adsorbed compounds 1, 2, 3, 4, or 5 with fine results.
- Costero, Ana M.,Parra, Margarita,Gil, Salvador,Gotor, Raffll,Mancini, Pedro M. E.,Martinez-Macez, Ramon,Sancenon, Felix,Royo, Santiago
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experimental part
p. 1573 - 1585
(2011/08/05)
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- Design, synthesis and identification of novel colchicine-derived immunosuppressant
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Synthesis and biological evaluation of various colchicine analogues through the mixed-lymphocyte reaction (MLR), lymphoproliferation, and inhibitory effects on the inflammatory genes are described. In addition, a new series of immunosuppressive agents developed on the structural basis of colchicine, as well as their structure-activity relationships is reported. The most potent analogue 20a exhibited an excellent immunosuppressive activity on in vivo skin-allograft model, which is comparable to that of cyclosporin A.
- Chang, Dong-Jo,Yoon, Eun-Young,Lee, Geon-Bong,Kim, Soon-Ok,Kim, Wan-Joo,Kim, Young-Myeong,Jung, Jong-Wha,An, Hongchan,Suh, Young-Ger
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scheme or table
p. 4416 - 4420
(2010/04/05)
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- Asymmetric total synthesis of martinelline and martinellic acid
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Herein, we describe the first asymmetric total synthesis of (-)-martinelline ((-)-2) and the second total synthesis of (-)-martinellic acid ((-)-1) by employing a tandem Mukaiyama-Mannich reaction/aminal cyclization as the key step. The Royal Society of C
- Ikeda, Shuhei,Shibuya, Masatoshi,Iwabuchi, Yoshiharu
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p. 504 - 506
(2007/10/03)
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- O-nitrobenzyl photolabile protecting groups with red-shifted absorption: Syntheses and uncaging cross-sections for one- And two-photon excitation
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We evaluated the o-nitrobenzyl platform for designing photolabile protecting groups with red-shifted absorption that could be photolyzed upon one- and two-photon excitation. Several synthetic pathways to build different conjugated o-nitrobenzyl backbones,
- Aujard, Isabelle,Benbrahim, Chouaha,Gouget, Marine,Ruel, Odile,Baudin, Jean-Bernard,Neveu, Pierre,Jullien, Ludovic
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p. 6865 - 6879
(2007/10/03)
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- Facile Synthesis of Novel Nonpeptide Angiotensin II Receptor Antagonists
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A series of Losartan analogues 1-12 with different functional groups were synthesized and characterized. In comparison with the previous reports, the synthetic procedures described in this paper have been optimized as follows below: 1) preparation of aromatic amine 15 and 18 through hydrogenation by employing Raney Ni and hydrazine as catalysts in place of palladium; 2) preparation of nitro-compound 17 by using pure fuming nitric acid at -20 - -15°C; 3) alkylation of 21 with 22 or 23 in the presence of sodium hydride in place of potassium tert-butylate; 4) preparation of carboxylic acid 4 by ester cleavage rather than hydrolysis of cyano group.
- Yang, Ling-Chun,Qi, Chuan-Min,Zhang, Guan-Xin,Zou, Nan-Zhi
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p. 1107 - 1112
(2007/10/03)
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- Use of certain amides as probes for detection of antitubulin activity and resistance monitoring
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This invention relates to methods for screening compounds for antitubulin activity, evaluation of cells for sensitivity to antitubulin drugs, resistance monitoring and quantifying tubulin using certain amides that inhibit the growth of eukaryotic cells as
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- Process for the manufacture of acetonylbenzamides
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Novel routes for the preparation of acetonylbenzamides are provided by the reaction of an amine and acyl chloride. Novel routes to various intermediates used in the manufacture of acetonylbenzamides are also disclosed.
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- Fungicidically active N-acetonylbenzamide compounds
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Novel N-acetonylbenzamides are disclosed. These compounds are useful in controlling phytopathogenic fungi.
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- Methods for controlling algae
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A method for controlling algae and marine fouling organisms is described. The method employs N-acetonylbenzamides compounds provided in an effective amount to kill or inhibit the growth of the algae or fouling organisms.
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- Process for the manufacture of acetonylbenzamides
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Novel routes for the preparation of acetonylbenzamides are provided by the reaction of an amine and acyl chloride. Novel routes to various intermediates used in the manufacture of acetonylbenzamides are also disclosed.
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- Method for inhibiting the growth of mammalian cells
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A method for inhibiting mammalian cell growth is disclosed. The method uses compounds known as N-acetonylarylamides. The compounds have been shown to inhibit cell mitosis and to inhibit microtubule assembly. The method may be used to treat diseases associated with rapid cell growth, particularly cancer. The compounds used in the method of the present invention may be used in combination with other therapies and may be administered by known techniques for drug administration.
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- Method for controlling algae
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A method for controlling algae and marine fouling organisms is described. The method employs N-acetonylbenzamides compounds provided in an effective amount to kill or inhibit the growth of the algae or fouling organisms.
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- Method for treating protozoal infections
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A method for treating protozoal infections is described. The method employs N-acetonylbenzamide compounds provided in an effective amount to inhibit the growth of protozoans. The compounds are useful in controlling such protozoan parasites as Giardia lamb
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- Thromboxane A2 synthetase inhibitors with histamine H1-blocking activity: Synthesis and evaluation of a new series of indole derivatives
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A novel series of N-substituted 3-(1H-imidazol-1-ylmethyl)indole carboxylic acid derivatives were prepared and evaluated for thromboxane A2 (TXA2) synthetase-inhibitory and histaminergic H1-blocking activity. Among the compounds synthesized, indole-6-carboxylic acid derivatives showed higher activities than the other positional isomers of carboxylic acid. 1-[3-(4- Benzhydryl-1-piperazinyl)propyl]-3-(1H-imidazol-1-ylmethyl)-1H-indole-6- carboxylic acid (12) had the strongest thromboxane synthetase inhibitory activity (IC50 = 5 x 10-8 M) and H1-blocking activity (IC50 = 8 x 10- 9 M).
- Kamiya,Matsui,Shirahase,Nakamura,Wada,Kanda,Shimaji,Kakeya
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p. 1692 - 1695
(2007/10/03)
-
- Chemical process for the preparation of 3-alkylated indole
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A process for the preparation of a 3-alkylated indole, which comprises: a) reacting a N-(2-nitrostyryl) enamine with an alkylating agent to afford an imine salt, b) optionally reacting the imine salt with water to afford a (2-nitrophenyl)acetaldehyde, and c) reacting the imine salt or the (2-nitrophenyl)acetaldehyde with a reducing agent capable of selectively reducing the nitro group, to afford the desired 3-alkylated indole.
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- Carbamoyl derivatives
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The present invention concerns novel carbamoyl derivatives of formula I, set out herein, which antagonize the pharmacological actions of one or more of the arachidonic acid metabolites known as leukotrienes, making them useful whenever such antagonism is desired, such as in the treatment of those diseases in which leukotrienes are implicated, for example, in the treatment of allergic or inflammatory diseases, or of endotoxic or traumatic shock conditions. The invention also provides pharmaceutical compositions containing the novel derivatives for use in such treatments, methods for their use and processes and intermediates for the manufacture of the novel derivatives.
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- GRIGNARD REAGENTS SELECTIVE ATTACK TO NITROARENIC FUNCTION IN THE PRESENCE OF OTHER ELECTROPHILIC GROUPS
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Exclusive alkylation of the nitroarenic system takes place in competitive reactions of RMgX with nitrobenzene and various electrophiles such as ketones, esters, cyanoand iodo-derivatives and in reactions with some functionalized nitrobenzenes, only aldehy
- Bartoli, G.,Bosco, M.,Dalpozzo, R.
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p. 115 - 118
(2007/10/02)
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- Anovulatory method and chicken feed compositions
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2-(Substituted phenylimino)imidazolidines delay the onset of egg production in young pullets and inerrupt egg production in mature hens and are useful in producing an artificial molt.
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