- DIPHENYLUREA COMPOUND DERIVATIVE
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To provide a novel diphenylurea compound derivative that is involved in the functional regulation of an ion transporter of a plant.SOLUTION: The present invention relates to a diphenylurea compound derivative represented by the following formula (1) (each
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Paragraph 0050-0051
(2021/02/25)
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- IRIDIUM COMPLEX COMPOUND, COMPOSITION CONTAINING THE COMPOUND AND SOLVENT, ORGANIC ELECTROLUMINESCENT ELEMENT CONTAINING THE COMPOUND, DISPLAY DEVICE, AND ILLUMINATION DEVICE
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Provided is an iridium complex compound represented by formula (1) below. [Ir is an iridium atom. C1 to C6 are carbon atoms. N1 and N2 are nitrogen atoms. R1 to R4 are each a hydrogen atom
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Paragraph 0305; 0333; 0341-0342
(2020/11/27)
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- FUNCTION CONTROL AGENT FOR PLANT POTASSIUM ION TRANSPORTER, AND METHOD OF GROWING PLANT
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PROBLEM TO BE SOLVED: To provide: a function control agent for a plant potassium ion transporter by screening diphenylurea compound derivatives having function control activity targeting a transporter of a plant; and a method of growing a plant body modif
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Paragraph 0037
(2019/09/18)
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- Stable and reusable nanoscale Fe2O3-catalyzed aerobic oxidation process for the selective synthesis of nitriles and primary amides
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The sustainable introduction of nitrogen moieties in the form of nitrile or amide groups in functionalized molecules is of fundamental interest because nitrogen-containing motifs are found in a large number of life science molecules, natural products and materials. Hence, the synthesis and functionalization of nitriles and amides from easily available starting materials using cost-effective catalysts and green reagents is highly desired. In this regard, herein we report the nanoscale iron oxide-catalyzed environmentally benign synthesis of nitriles and primary amides from aldehydes and aqueous ammonia in the presence of 1 bar O2 or air. Under mild reaction conditions, this iron-catalyzed aerobic oxidation process proceeds to synthesise functionalized and structurally diverse aromatic, aliphatic and heterocyclic nitriles. Additionally, applying this iron-based protocol, primary amides have also been prepared in a water medium.
- Murugesan, Kathiravan,Senthamarai, Thirusangumurugan,Sohail, Manzar,Sharif, Muhammad,Kalevaru, Narayana V.,Jagadeesh, Rajenahally V.
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supporting information
p. 266 - 273
(2018/01/12)
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- Synthesis, characterization, and SAR of arylated indenoquinoline-based cholinesterase and carbonic anhydrase inhibitors
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We report the synthesis of bromoindenoquinolines (15a–f) by Friedlander reactions in low yields (13–50%) and the conversion of the corresponding phenyl-substituted indenoquinoline derivatives 16–21 in high yields (80–96%) by Suzuki coupling reactions. To explore the structure–activity relationship (SAR), their inhibition potentials to inhibit acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and human carbonic anhydrase cyctosolic (hCA I and II) enzymes were determined. Monophenyl (16–18) indenoquinolines significantly inhibited the AChE and BChE enzymes in ranges of IC50 37–57 nM and 84–93 nM, respectively, compared with their starting materials 15a–c and reference compounds (galanthamine and tacrine). On the other hand, these novel arylated indenoquinoline-based derivatives were effective inhibitors of the BChE, hCA I and II, BChE and AChE enzymes with Ki values in the range of 37 ± 2.04 to 88640 ± 1990 nM for AChE, 120.94 ± 37.06 to 1150.95 ± 304.48 nM for hCA I, 267.58 ± 98.05 to 1568.16 ± 438.67 nM for hCA II, and 84 ± 3.86 to 144120 ± 2910 nM for BChE. As a result, monophenyl indenoquinolines 16–18 may have promising anti-Alzheimer drug potential and 3,8-dibromoindenoquinoline amine (15f) can be novel hCA I and hCA II enzyme inhibitors.
- Ekiz, Makbule,Tutar, Ahmet,?kten, Salih,Bütün, Burcu,Ko?yi?it, ümit M.,Taslimi, Parham,Top?u, Güla?t?
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- SELECTIVE INHIBITORS OF CLINICALLY IMPORTANT MUTANTS OF THE EGFR TYROSINE KINASE
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The present invention provides compounds of Formula (I) or a subgeneric structure or species thereof, or a pharmaceutically acceptable salt, ester, solvate, and/or prodrug thereof, and methods and compositions for treating or ameliorating abnormal cell proliferative disorders, such as cancer, wherein A, R2, R3, R10, E1, E2, E3, Y, and Z are as defined herein.
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Page/Page column 304
(2017/08/01)
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- Convenient synthesis of disubstituted tacrine derivatives via electrophilic and copper induced reactions
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The bromination of 2-aminobenzonitrile (2) with molecular bromine (2?equiv) furnished 2-amino-3,5-dibromobenzonitrile (7) in 98% yield. One-pot syntheses are described for dibromotacrine derivatives (6, 14–18) utilizing Friedl?nder reactions. A convenient route is described for disubstituted derivatives of tacrines from dibromotacrine 6 and 15 by various substitution reactions. Several disubstituted tacrines were synthesized by treatment of dibromo 6 and 15 derivatives with n-BuLi followed by trapping with an electrophile [Si(Me)3Cl, S2(Me)2]. Both were converted to the corresponding cyano derivatives (21–23) via copper-assisted nucleophilic substitution reactions in moderate yields (30%, 50%, and 60%, respectively). Copper-induced nucleophilic substitution of dibromide 15 with NaOMe afforded mono methoxide 31 in 25% yield.
- Ekiz, Makbule,Tutar, Ahmet,?kten, Salih
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p. 5323 - 5330
(2016/08/05)
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- Efficient access to 2,6,8-trisubstituted 4-aminoquinazolines through microwave-assisted one-pot chemoselective Tris-Suzuki-Miyaura or SNAr/bis-Suzuki-Miyaura reactions in water
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An efficient, sequential, one-pot strategy for synthesizing polyfunctionalized quinazoline derivatives is presented. After selective amination of 6,8-dibromo-2,4-dichloroquinazoline at the C-4 position, 2,6,8-trisubstituted 4-aminoquinazoline derivatives
- Kabri, Youssef,Crozet, Maxime D.,Terme, Thierry,Vanelle, Patrice
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supporting information
p. 3806 - 3817
(2015/06/16)
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- An electroluminescent compound and an electroluminescent device comprising the same
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The present invention relates to organic light emitting compounds represented by chemical formula 1-1 to chemical formula 1-2. An organic electroluminescent device using the same has excellent light emitting efficiency and can be driven at low voltage, thereby having improved power efficiency and long life characteristics.COPYRIGHT KIPO 2015
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Paragraph 0604-0610
(2020/12/25)
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- One-pot chemoselective synthesis of 2,4,6,8-tetrasubstituted quinazolines via microwave-assisted consecutive bis-SNAr/Bis-Suzuki-Miyaura cross-coupling reactions
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A practical and efficient synthesis of 2,4,6,8-tetrasubstituted quinazolines through one-pot chemoselective sequential bis-SNAr/bis- Suzuki-Miyaura reactions under microwave irradiation is presented. The bis-SNAr reaction occurs selectively at the C-2 and C-4 positions of 6,8-dibromo-2,4-dichloroquinazoline and the bis-Suzuki-Miyaura cross-coupling at C-6 and C-8. This procedure affords convergent synthesis of polysubstituted quinazoline derivatives in high yields in very few steps and tolerates a wide range of boronic acids and amines.
- Kabri, Youssef,Crozet, Maxime D.,Redon, Sebastien,Vanelle, Patrice
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p. 1613 - 1620
(2014/06/23)
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- Fast and efficient bromination of aromatic compounds with ammonium bromide and Oxone
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A highly efficient, rapid and regioselective protocol was developed for the ring bromination of aromatic compounds under mild conditions with ammonium bromide as a source of bromine source and Oxone (potassium peroxysulfate) as an oxidant. No metal catalyst or acidic additive is required. A variety of aromatic compounds, including methoxy, hydroxy, amino, and alkyl arenes, reacted smoothly to give the corresponding monobrominated products in good to excellent yields in very short reaction times. Moreover, dibromination of deactivated anilines to give the corresponding dibromides proceeded in high yields. Interestingly, 1-(2-naphthyl)ethanone provided a ring-brominated product. Georg Thieme Verlag Stuttgart . New York.
- Naresh, Mameda,Arun Kumar, Macharla,Mahender Reddy, Marri,Swamy, Peraka,Nanubolu, Jagadeesh Babu,Narender, Nama
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p. 1497 - 1504
(2013/06/27)
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- An efficient regioselective NBS aromatic bromination in the presence of an ionic liquid
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A simple, efficient, and rapid method was developed for high-yielding regioselective monobromination of activated aromatic compounds using NBS in combination with ionic liquid 1-butyl-1-methylimidazolium bromide ([Bmim]Br) or dioxane. The ionic liquid is recyclable and can be reused with minimal loss in the catalytic efficiency if the ionic liquid is rapidly microwaved prior to reactions.
- Pingali, Subramanya R.K.,Madhav, Monika,Jursic, Branko S.
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experimental part
p. 1383 - 1385
(2010/04/25)
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- Synthesis of benzotriazine and aryltriazene derivatives starting from 2-azidobenzonitrile derivatives
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3-Substituted 3,4-dihydro-4-imino-1,2,3-benzotriazine derivatives 7 were formed from 2-azidobenzonitriles 4 as starting materials on treatment with Grignard or lithium organic reagents. In some cases these procedures gave aryltriazenes 10 and 11 as products. All compounds were identified by NMR spectroscopy and the structures of three products, namely 7a, 10a and 11i, were corroborated by X-ray crystallography. The reactions of 2-azidobenzonitrile derivatives with Grignard reagents have been investigated. These reactions, depending on the type of Grignard reagent and the substituents on the 2-azidobenzonitrile derivatives, resulted in benzotriazines and triazenes. Copyright
- Nakhai, Azadeh,Stensland, Birgitta,Svensson, Per H.,Bergman, Jan
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experimental part
p. 6588 - 6599
(2011/02/26)
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- EPR studies of nitrogen-centred free radicals. Part 53. Isolation, EPR spectra and magnetic characterization of N-(arylthio)-2,4-diaryl-6-cyanophenylaminyls
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N-(Arylthio)-2,4-diaryl-6-ethoxycarbonylphenylaminyls (1), N-[(2,4-dichlorophenyl)thio]-2,4-diphenyl-6-acetylphenylaminyl (2), N-(arylthio)-2,4-diaryl-6-cyanophenylaminyls (3), N-[(2,4-dichlorophenyl)thio]-2,4-bis(4-chlorophenyl)-6-fluorophenylaminyl (4) and N-[(4-nitrophenyl)thio]-2,4-diphenylphenylaminyl (5) were generated by oxidation of the corresponding N-(arylthio)anilines. Although 4 and 5 were short-lived and decayed in 30 min, 1-3 were quite persistent and 3 could be isolated as radical crystals. EPR spectra were measured for all radicals generated and the spin density distribution was evaluated. Ab initio MO calculations (the UHF Becke 3LYP/STO 6-31G) were performed, and a quantitative discussion on the spin density distribution was made. Magnetic susceptibility measurements were performed for three isolated radicals with a SQUID magnetometer. One radical was found to couple ferromagnetically, and analysis with the one-dimensional regular Heisenberg model gave 2J/kB = 11.2 K.
- Nakatsuji, Masaaki,Miura, Yozo,Teki, Yoshio
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p. 738 - 744
(2007/10/03)
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- Mild and regioselective oxidative bromination of anilines using potassium bromide and sodium perborate
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The selective monobromination of various deactivated anilines using potassium bromide and sodium perborate as oxidant has been achieved. The use of ammonium molybdate as catalyst accelerates the rate of reaction but is not essential to obtain good yields and high selectivities. (C) 2000 Elsevier Science Ltd.
- Roche, Didier,Prasad, Kapa,Repic, Oljan,Blacklock, Thomas J.
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p. 2083 - 2085
(2007/10/03)
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- Pyrolysis of Aryl Azides. V. Characterization of Phenylazo, Benzoyl and Formyl as Neighbouring Groups
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The enhancements of thermolysis rate of azidobenzene produced by ortho phenylazo, benzoyl and formyl substituents are 21180, 70.0 and 22.8 at 393.2 K (decalin solutions).The same ortho substituents produce much smaller enhancements (169, 8.56 and 10.7 respectively) in the pyrolysis rate of 1-azido-2,4-dibromobenzene.These results are interpreted as steric effects on an electrocyclic thermolysis mechanism, and are not consistent with the alternative pathway of intramolecular 1,3-dipolar addition which continues to be advocated by Hall and Dolan.
- Dickson, Noel J.,Dyall, Leonard K.
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- Compositions and process of treatment
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This invention relates to pharmaceutical compositions containing known compounds of the formula SPC1 Wherein M is selected from the group consisting of hydrogen, aluminum, ammonium, sodium, potassium, calcium, tris(hydroxymethyl)methylammonium and lower alkyl of 1 through 4 carbon atoms, R is selected from the group consisting of hydrogen and lower alkyl of 1 through 4 carbon atoms, and R1 and R2 are selected from the group consisting of hydrogen, fluorine, chlorine, bromine, trifluoromethyl, lower alkoxy of 1 through 4 carbon atoms and lower alkyl of 1 through 4 carbon atoms. The compounds (1) above are formulated with pharmaceutical carriers for inhalation or for oral, parenteral or rectal administration, with insufflation being the preferred method. The compositions are useful in the prophylactic treatment of sensitized humans and mammals for allergic and all anaphylactic reactions of a reaginmediated and non-reagin-mediated nature.
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