63010-73-1Relevant academic research and scientific papers
Facile one-pot multicomponent synthesis of highly functionalized tetrahydropyridines using thiamine hydrochloride as an organocatalyst
Singh, Sandeep,Gupta, Annah,Kapoor, Kamal K.
supporting information, p. 1056 - 1063 (2020/03/04)
Thiamine hydrochloride (VitB1) has been found to be an efficient catalyst for the multicomponent synthesis of highly functionalized tetrahydropyridines from the reaction of β-ketoester, aromatic aldehydes and anilines. VitB1 is easily available, cheap, and eco benign.
Antibacterial activity and fluorescence properties of 4,7-dichloro-2-quinolinemethylacrylate
Aguilar, Luis,Carrasco, Carlos,Dahrouch, Mohamed,Padilla, Natalia,Rivas, Bernabé,Urrutia, Homero,Valle, Hernán,Viswanathan Mangalaraja, Ramalinga
, p. 4784 - 4789 (2020/09/16)
Currently, some quinoline-based anticancer drugs are successful repurposed for treatment of bacterial infections. This study assessed the antibacterial activity of the new anticancer compound 4,7-dichloro-2-quinolinemethylacrylate (AQM) against bacteria o
Synthesis of 3 H -Pyrrolo[2,3- c ]quinoline by Sequential i 2 -Promoted Cyclization/Staudinger/Aza-Wittig/Dehydroaromatization Reaction
Zou, Fakai,Pei, Fei,Wang, Liping,Ren, Zhilin,Cheng, Xiaohong,Sun, Yang,Wu, Jing,He, Ping
, p. 717 - 720 (2019/03/26)
A facile synthetic approach to access of 3 H -pyrrolo[2,3- c ]quinoline derivatives has been achieved by a sequential I 2 -promoted cyclization/Staudinger/aza-Wittig/dehydroaromatization reaction. The targeted products were received in moderate
Graphene oxide: A carbocatalyst for the one-pot multicomponent synthesis of highly functionalized tetrahydropyridines
Gupta, Annah,Kaur, Ramneet,Singh, Deepika,Kapoor, Kamal K.
, p. 2583 - 2587 (2017/06/13)
A simple, straightforward and efficient methodology is described for the synthesis of polysubstituted tetrahydropyridine via one-pot multicomponent reaction of β-ketoester, aldehyde and aniline in presence of catalytic amount of graphene oxide in acetonitrile. Graphene oxide is a versatile carbocatalyst and this is the first report on its application in a five component reaction. Good yield, usage of readily available starting material, operational simplicity, easy work-up and eco-friendly re-usable catalyst are the key features of this protocol.
N1-{4-[(10S)-Dihydroartemisinin-10-oxyl]}phenylmethylene-N 2-(2-methylquinoline-4-yl)hydrazine derivatives as antiplasmodial falcipain-2 inhibitors
Luo, Wei,Liu, Yang,Wang, Jian,Guo, Chun,Lu, Wei-Qiang,Cui, Kun-Qiang
, p. 3073 - 3079,7 (2020/08/20)
A series of N1-{4-[(10S)-dihydroartemisinin- 10-oxyl]}phenylmethylene-N2-(2-methylquinoline-4-yl) hydrazine derivatives 9a-9n possessing 4-quinolylhydrazone and artemisinin cores were herein synthesized and evaluated for their activities against cysteine protease falcipain- 2 of Plasmodium falciparum. The structures were clearly confirmed by elemental analysis, 1H NMR, and mass spectra. The pharmacological results indicated that all compounds showed excellent activity against recombinant falcipain-2 (IC50 = 0.15-2.28 μM). The best one of this series was compound 9d (IC50 = 0.15 μM). The molecular docking results showed that the compound 9d made close contact with the key active site of cysteine protease falcipain-2.
Cyanuric chloride catalysed rapid conversion of β-ketoesters into β-enaminoesters under mild and solvent-free conditions
Kamble,Joshi,Atkore
experimental part, p. 616 - 621 (2012/07/03)
Cyanuric chloride is shown to be an extremely efficient catalyst for the synthesis of β-enaminoesters from β-ketoesters under solvent-free conditions by grinding in a mortar with pestle at 25 °C. A short reaction time, an inexpensive and easily available catalyst, mild reaction conditions and excellent yields of the products are attractive features of this methodology.
B2O3/Al2O3 as a new, highly efficient and reusable heterogeneous catalyst for the selective synthesis of β-enamino ketones and esters under solvent-free conditions
Chen, Jiu-Xi,Zhang, Chang-Fu,Gao, Wen-Xia,Jin, Hui-Le,Ding, Jin-Chang,Wu, Hua-Yue
experimental part, p. 1552 - 1556 (2010/11/16)
Boron oxide adsorbed on alumina (B2O3/Al 2O3) has been found to be a new and highly efficient heterogeneous catalyst for the synthesis of β-enamino ketones and esters by the enamination of various primary and secondary amines with β-dicarbonyl compounds under solvent-free conditions. The important features of this methodology are broad substrate scope, high yield, no requirement of metal catalysts, high regio-and chemoselectivity and environmental friendliness. In addition, the catalyst could be recovered easily after the reactions and reused without evident loss of reactivity.
Synthesis and biological screening of some new novel indole derivatives
Mehta,Sikotra,Shah
, p. 2594 - 2597 (2007/10/03)
Synthesis of some novel indole derivatives has been undertaken by the reaction of 1,4-benzoquinone with ethyl-β-(arylamino)-crotonates in the presence/absence of nitrogen atmosphere. The products 1a-o have been screened for their antimicrobial activity an
Antimalarials: Synthesis of 4-aminoquinolines that circumvent drug resistance in malaria parasites
De,Byers,Krogstad
, p. 315 - 320 (2007/10/03)
The strategies described here have permitted the synthesis of a series of 4-aminoquinoline antimalarials. Substantive improvements over previous syntheses include nucleophilic substitution with neat amine rather than in phenol, regioselective reductive alkylation to convert the terminal primary amine (12a-20a) on the diaminoalkane side chain to a diethylamino group, and purification by column chromatography with basic alumina. The 1H nmr spectra obtained after regioselective reductive alkylation with sodium borodeuteride (in comparison with sodium borohydride) demonstrated that this reductive alkylation proceeds via formation and subsequent reduction of the corresponding diamides in situ.
Synthesis of (E)-2-(4,7-dichloroquinolin-2-yl)-3-dimethylamino-2-propene-1-al and its use as a synthetic intermediate
De, Dibyendu,Mague, Joel T.,Byers, Larry D.,Krogstad, Donald J.
, p. 205 - 208 (2007/10/02)
A novel synthesis is described for (E)-2-(4,7-dichloroquinolin-2-yl)-3-dimethylamino-2-propene-1-al (4), which reacts with nucleophiles to yield heterocycle-substituted 4,7-dichloroquinolines (5-7).
