1047680-82-9Relevant academic research and scientific papers
A new solvent-free synthesis of α,β-unsaturated ketones from acetals with aryl ketones under microwave irradiation
Huang, Danfeng,Wang, Jin-Xian,Hu, Yulai,Zhang, Yumei,Tang, Jing
, p. 971 - 979 (2002)
A new, rapid and efficient method for the synthesis of α,βunsaturated ketones under microwave irradiation conditions is described. The process involves the reaction of acetals with aryl ketones in the absence of solvent using Lewis acids as catalysts under microwave irradiation to afford the α,βunsaturated ketones in good to excellent isolated yields. The reaction mechanism is briefly discussed.
Synthesis method of chalcone derivative
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Paragraph 0075-0077; 0081; 0082; 0089, (2020/07/03)
The invention provides a synthesis method of a chalcone derivative, which comprises the following steps: adding polyphosphoric acid PPA and a solvent 1, 4-dioxane into a container, sequentially adding98% concentrated sulfuric acid, substituted benzaldehyd
An eco-friendly synthesis of 2-pyrazoline derivatives catalysed by CeCl 3· 7 H 2O
Bhat, Prabhat,Shridhar, Gomathi,Ladage, Savita,Ravishankar, Lakshmy
, p. 1441 - 1448 (2017/09/25)
Abstract: 1,3,5-triaryl-2-pyrazoline derivatives were synthesised by a condensation reaction between chalcones and phenyl hydrazine using cerium chloride heptahydrate as a catalyst. All these reactions were carried out in ethyl lactate (70%) as a green solvent. Easy and efficient work up, recyclability of solvent and catalyst are the key merits of this protocol. Graphical Abstract:: SYNOPSIS A facile protocol for the synthesis of 1,3,5-triaryl-2-pyrazolines is described. The solvent ethyl lactate, obtained from renewable sources, is biodegradable. The catalyst CeCl 3· 7 H 2O is a water-tolerant Lewis acid with low toxicity. Easy and clean work up, recyclable solvent and catalyst are merits of the protocol. The reaction works well for all systems giving good yields of the desired products.[Figure not available: see fulltext.].
Antimycobacterial and anti-inflammatory activities of substituted chalcones focusing on an anti-tuberculosis dual treatment approach
Ventura, Thatiana Lopes Biá,Calixto, Sanderson Dias,De Azevedo Abrahim-Vieira, Bárbara,De Souza, Alessandra Mendon?a Teles,Mello, Marcos Vinícius Palmeira,Rodrigues, Carlos Rangel,De Mariz E Miranda, Leandro Soter,De Souza, Rodrigo Octavio Mendon?a Alves,Leal, Ivana Correa Ramos,Lasunskaia, Elena B.,Muzitano, Michelle Fraz?o
, p. 8072 - 8093 (2015/05/20)
Tuberculosis (TB) remains a serious public health problem aggravated by the emergence of M. tuberculosis (Mtb) strains resistant to multiple drugs (MDR). Delay in TB treatment, common in the MDR-TB cases, can lead to deleterious life-threatening inflammation in susceptible hyper-reactive individuals, encouraging the discovery of new anti-Mtb drugs and the use of adjunctive therapy based on anti-inflammatory interventions. In this study, a series of forty synthetic chalcones was evaluated in vitro for their anti-inflammatory and antimycobacterial properties and in silico for pharmacokinetic parameters. Seven compounds strongly inhibited NO and PGE2 production by LPS-stimulated macrophages through the specific inhibition of iNOS and COX-2 expression, respectively, with compounds 4 and 5 standing out in this respect. Four of the seven most active compounds were able to inhibit production of TNF-α and IL-1β. Chalcones that were not toxic to cultured macrophages were tested for antimycobacterial activity. Eight compounds were able to inhibit growth of the M. bovis BCG and Mtb H37Rv strains in bacterial cultures and in infected macrophages. Four of them, including compounds 4 and 5, were active against a hypervirulent clinical Mtb isolate as well. In silico analysis of ADMET properties showed that the evaluated chalcones displayed satisfactory pharmacokinetic parameters. In conclusion, the obtained data demonstrate that at least two of the studied chalcones, compounds 4 and 5, are promising antimycobacterial and anti-inflammatory agents, especially focusing on an anti-tuberculosis dual treatment approach.
Iron-catalyzed aerobic oxidative aromatization of 1,3,5-trisubstituted pyrazolines
Ananthnag, Guddekoppa S.,Adhikari, Adithya,Balakrishna, Maravanji S.
, p. 240 - 243 (2013/12/04)
A simple and high yielding method for the synthesis of tri-substituted pyrazoles via iron(III) catalyzed aerobic oxidative aromatization of pyrazolines has been reported. The process demonstrates a variety of functional group tolerance.
Synthesis, characterization, and anti-amoebic activity of N-(pyrimidin-2-yl)benzenesulfonamide derivatives
Roouf Bhat, Abdul,Arshad, Mohammad,Ju Lee, Eun,Pokharel, Smritee,Choi, Inho,Athar, Fareeda
, p. 2267 - 2277 (2014/01/06)
A new series of N-(pyrimidin-2-yl)benzenesulfonamide derivatives, 3a-3i and 4a-4i, was synthesized from pyrimidin-2-amines, 2a-2i, with the aim to explore their effects on in vitro growth of Entamoeba histolytica. The chemical structures of the compounds
Synthesis of chalcones with anticancer activities
Syam, Suvitha,Abdelwahab, Siddig Ibrahim,Al-Mamary, Mohammed Ali,Mohan, Syam
experimental part, p. 6179 - 6195 (2012/09/07)
Several chalcones were synthesized and their in vitro cytotoxicity against various human cell lines, including human breast adenocarcinoma cell line MCF-7, human lung adenocarcinoma cell line A549, human prostate cancer cell line PC3, human adenocarcinoma cell line HT-29 (colorectal cancer) and human normal liver cell line WRL-68 was evaluated. Most of the compounds being active cytotoxic agents, four of them with minimal IC50 values were chosen and studied in detail with MCF-7 cells. The compounds 1, 5, 23, and 25 were capable in eliciting apoptosis in MCF-7 cells as shown by multiparameter cytotoxicity assay and caspase-3/7, -8, and -9 activities (p 0.05). The ROS level showed 1.3-fold increase (p 0.05) at the low concentrations used and thus it was concluded that the compounds increased the ROS level eventually leading to apoptosis in MCF-7 cells through intrinsic as well as extrinsic pathways.
A palladium catalyzed atom-efficient cross-coupling reactivity of triarylbismuths with α,β-unsaturated acyl chlorides
Rao, Maddali L.N.,Venkatesh, Varadhachari,Jadhav, Deepak N.
, p. 2494 - 2498 (2008/09/21)
An atom-efficient cross-coupling reactivity of triarylbismuths (1 equiv) was demonstrated by cross-coupling reaction with 3 equiv of α,β-unsaturated acyl chlorides under palladium catalysis in the synthesis of a series of functionalized α, β-unsaturated ketones in high isolated yields.
