- Organometallic titanocene complex as highly efficient bifunctional catalyst for intramolecular Mannich reaction
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Bifunctional catalysts bearing two catalytic sites, Lewis acidic organometallic titanocene and Br?nsted acidic COOH, have been assembled in situ from Cp2TiCl2 with carboxylic acid ligands, showing high catalytic activity over an intramolecular Mannich reaction towards synthesis of 2-aryl-2,3-dihydroquinolin-4(1H)-ones. The determination of the bifunctional catalyst Cp2Ti(C8H4NO6)2 was elucidated by single X-ray HR-MS and investigation of catalytic behavior. In particular, masking the Br?nsted acidic COOH catalytic site with dormant COOMe lowered the reaction yield greatly, indicating that two catalytic sites work together to maintain high catalytic efficiency.
- Wang, Yunyun,Jian, Yajun,Wu, Ya,Sun, Huaming,Zhang, Guofang,Zhang, Weiqiang,Gao, Ziwei
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- Titanocene complex with oxygen-containing carboxylic acid as ligand as well as preparation method and application of titanocene complex
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The invention discloses a titanocene complex with oxygen-containing carboxylic acid as well as a preparation method and an application of the titanocene complex. The structural formula of the complexis shown in the description. The titanocene complex is p
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Paragraph 0039; 0040; 0042
(2018/11/03)
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- 2-aryl-2,3-dihydro-4(1H)-quinolinone semicarbazone compound and application thereof
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The invention relates to the field of medicine technology, and a series of novel 2-aryl-2,3-dihydrogen-4(1H)-quinolinone semicarbazone derivatives (I) and pharmaceutically acceptable salts, solvates,optical isomers or polymorphs are designed and synthesized. The derivative (I) and its pharmaceutically acceptable salt, solvate, optical isomer or polymorph can be mixed as an active ingredient witha pharmaceutically acceptable carrier to prepare a pharmaceutical composition. A double dilution method is used for test of the antifungal activity of the derivative (I) and its pharmaceutically acceptable salt, solvate, optical isomer or polymorph, and the results show that the derivative has stronger killing effect on clinically common pathogenic fungi, and is expected to overcome the defects oflarge toxic and side effects, easy generation of drug resistance of azole antifungal medicines which are widely used clinically. The specific formula is shown in the description.
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Paragraph 0071; 0072; 0073; 0074; 0075; 0076
(2018/10/19)
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- Zirconyl Nitrate as an Efficient Catalyst for Facile Synthesis of 2-Aryl-2,3-dihydroquinolin-4(1 H)-one Derivatives in Aqueous Medium
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A simple, green, and efficient method is introduced for the synthesis of 2-aryl-2,3-dihydroquinolin-4(1 H)-ones under mild reaction conditions with improved yields by intramolecular cyclization of o -aminochalcones with zirconyl nitrate [Zn(O)(NO 3/
- Gorepatil, Amarsinha,Gorepatil, Pratapsinha,Gaikwad, Mahadev,Mhamane, Dattakumar,Phadkule, Ajit,Ingle, Vilas
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p. 235 - 237
(2017/09/28)
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- Synthesis, molecular modeling and biological evaluation of aza-flavanones as α-glucosidase inhibitors
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An efficient acid catalyzed methodology has been employed to synthesize a variety of aza-flavanones and their α-glucosidase inhibitory activity is evaluated using acarbose, miglitol and voglibose as reference standards. Molecular modeling studies were per
- Kasturi, Sivaprasad,Surarapu, Sujatha,Bathoju, Chandra Chary,Uppalanchi, Srinivas,Dwivedi, Shubham,Perumal, Yogeeswari,Sigalapalli, Dilep Kumar,Babu, Bathini Nagendra,Ethiraj, Krishna S.,Anireddy, Jaya Shree
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p. 1618 - 1630
(2017/08/22)
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- [C8dabco]Br: a mild and convenient catalyst for intramolecular cyclization of 2-aminochalcones to the corresponding 2-aryl-2,3-dihydroquinolin-4(1H)-ones
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[Figure not available: see fulltext.] A new and convenient synthesis of 2-aryl-2,3-dihydroquinolin-4(1H)-ones has been described using the intramolecular cyclization of 2-aminochalcones catalyzed by 1-octyl-4-aza-1-azoniabicyclo[2.2.2]octane bromide ([Cs
- Derabli, Chamseddine,Mahdjoub, Sara,Boulcina, Raouf,Boumoud, Boudjemaa,Merazig, Hocine,Debache, Abdelmadjid
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- A general and efficient synthesis of 5,6-dihydrodibenzo[b,h][1,6]naphthyridine derivatives
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A two-step procedure for the synthesis of dihydrodibenzonaphthyridine derivatives from benzaldehydes and 2-aminoacetophenones, proceeding through a substituted dihydroquinolone intermediate, is described. The synthetic protocol allows for a versatile and robust coupling method between a range of 2-aminoacetophenones or 2-aminobenzophenones and a selection of substituted dihydroquinolones.
- Dobrowolski, Jeremy C.,Katen, Alice,Fraser, Benjamin H.,Bhadbhade, Mohan,Black, David StC.,Kumar, Naresh
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p. 5442 - 5445
(2016/11/19)
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- Mild and Efficient Silver(I) Triflate Catalyzed Synthesis of 2-Aryl-2,3-dihydroquinolin-4(1 H)-ones, and Their Antioxidant Activities
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Biologically interesting 2-aryl-2,3-dihydroquinolin-4(1H)-ones were synthesized using a mild and efficient one-pot procedure starting from o-aminoacetophenones and aromatic aldehydes in the presence of silver(I) triflate. This synthetic protocol provides rapid access to a variety of 2-aryl-2,3-dihydroquinolin-4(1H)-ones. This technique has several advantages, such as the use of easily available starting materials, the efficiency of the catalyst, a simple operation, and tolerance of a wide range of functionality in the aldehydes. Screening of the synthesized compounds for their antioxidant properties revealed that two compounds (with EC50 = 15.42 μM and 15.16 μM) exhibit a potent free-radical scavenging ability towards TEAC free radicals compared to the standard, Trolox.
- Pandit, Rameshwar Prasad,Sharma, Kavita,Lee, Yong Rok
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p. 3881 - 3890
(2015/12/18)
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- Silica supported-double metal cyanides (DMCs): A green and highly efficient catalytic protocol for isomerisation of 2′-hydroxychalcones to flavanones
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Four different double metal cyanides (NiHCFe, CrHCFe, MnHCFe and ZnHCFe) were synthesized, followed by adsorbed on silica gel and used as Lewis acid catalyst in the isomerisation of substituted 2′-hydroxychalcones to flavanones under solvent-free (dry) condition. Optimization of the reaction condition, temperature effects, DMC catalysts loading and re-useable catalytic activity were further studied during the reaction. Among these catalysts, NiHCFe at 35 mol% loading gave excellent yield (90%) at 100 C temperature in 1.15 h. Catalyst (NiHCFe) easily recovered and re-used six times without much loss of its catalytic activity which gave 80-85% product yields each time. However, these DMCs were failed to give product in the solution phase even prolonging the reaction time at reflux temperature. Similarly, isomerization of substituted 2′-aminochalcones gave 2-5% yields either in solution phase or under solvent-free condition.
- Ahmed, Naseem,Konduru, Naveen Kumar,Praveen,Kumar, Anand,Kamaluddin
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p. 135 - 141
(2013/06/26)
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- An efficient and rapid intramolecular aza-Michael addition of 2′-aminochalcones using ionic liquids as recyclable reaction media
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A new, convenient, and efficient method for the intramolecular aza-Michael addition reaction of 2′-aminochalcones is developed using 1-n-butyl-3-methylimidazolium tetrafluoroborate as the solvent and catalyst. The ionic liquid is successfully regenerated and reused.
- Chelghoum,Bahnous,Bouraiou,Bouacida,Belfaitah
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experimental part
p. 4059 - 4061
(2012/08/28)
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- Aza-Flavanones as potent cross-species microRNA inhibitors that arrest cell cycle
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aza-Flavanones have been identified as a new class of selective microRNA inhibitors. These compounds were found to arrest cell cycle via a novel cross species microRNA-dependent regulatory pathway interpreting an unexpected link between cell cycle arrest and microRNA mediated control in cancer.
- Chandrasekhar, Srivari,Pushpavalli, Sreerangam N.C.V.L.,Chatla, Srinivas,Mukhopadhyay, Debasmita,Ganganna, Bogonda,Vijeender, Kandi,Srihari, Pabbaraja,Reddy, Chada Raji,Janaki Ramaiah,Bhadra, Utpal
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supporting information; experimental part
p. 645 - 648
(2012/03/26)
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- Alumina supported-CeCl3·7H2O-NaI: an efficient catalyst for the cyclization of 2′-aminochalcones to the corresponding 2-aryl-2,3-dihydroquinolin-4(1H)-ones under solvent free conditions
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We recently advanced silica gel supported-TaBr5 as an efficient catalyst for the isomerization of 2′-aminochalcones to the corresponding 2-aryl-2,3-dihydroquinolin-4(1H)-ones under solvent free conditions (Tetrahedron Lett. 2006, 47, 2725-2729)
- Ahmed, Naseem,van Lier, Johan E.
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- Silica gel supported TaBr5: New catalyst for the facile and rapid cyclization of 2′-aminochalcones to the corresponding 2-aryl-2,3-dihydroquinolin-4(1H)-ones under solvent-free conditions
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Silica gel supported TaBr5 (5-10 mol %) is a new solid-support catalyst that can be used under solvent-free conditions for the facile and efficient isomerization of 2′-aminochalcones to the corresponding 2-aryl-2,3-dihydroquinolin-4(1H)-ones. The catalyst is easily prepared, stable and employed under environmentally friendly conditions.
- Ahmed, Naseem,Van Lier, Johan E.
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p. 2725 - 2729
(2007/10/03)
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- Microwave-Assisted Isomerization of 2′-Aminochalcones on Clay: An Easy Route to 2-Aryl-1,2,3,4-tetrahydro-4-quinolones
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A simple and environmentally benign method for the conversion of 2′-aminochalcones to 2-aryl-1,2,3,4-tetrahydro-4-quinolones is described which occurs under mild and solvent-free conditions on montmorillonite K 10 clay surface; microwave irradiation facil
- Varma, Rajender S.,Saini, Rajesh K.
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p. 857 - 858
(2007/10/03)
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- Fragmentation pathways in the electron impact mass spectra of 2-aryl-1,2,3,4-tetrahydro-4-quinolones
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The major feagmentation pathways in the electron impact mass spectra of a series of 2-aryl-1,2,3,4-tetrahydro-4-quinolones have been determined using a combination of low- and high-resolution mass spectrometry and matastable peak analysis.
- Kaye, Perry T.,Mphahlele, M. Jack
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- N-heterocycles by cyclization of 2'-NHR-chalcones, 2'-NHR-chalcone dibromides and 2'-NHR-α-azidochalcones
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Syntheses of six-membered N-heterocycles from 2'-NHR-chalcones, 2'-NHR-chalcone dibromides and 2'-NHR-α-azidochalcones are described and discussed.
- Tokes,Litkei,Szilagyi
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p. 2433 - 2445
(2007/10/02)
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