70354-15-3Relevant academic research and scientific papers
Method for synthesizing 2-aryl benzopyrone flavonoid derivatives
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, (2019/04/30)
The invention relates to a method for synthesizing 2-aryl benzopyrone flavonoid derivatives, and relates to a method for synthesizing a compound, the method for synthesizing 2-aryl benzopyrone flavonoid derivatives is suitable for the synthesis of 2-aryl benzopyrone flavonoid derivatives containing different substituents. The method aims to solve the technical problems of low yield, long reactionperiod, and complicated post-treatment and high operation difficulty of the existing synthesis method of the ketone flavonoid derivative. The method comprises the following steps of: 1, preparing beta-propanedione compounds; 2, preparing flavonoid compound 2-aryl benzopyranones. The method completes esterification and rearrangement in one step, which is simple and practical, reduces intermediate links of reaction, saves separation and purification of intermediate products, improves utilization rate of raw materials, reduces reaction temperature, shortens reaction time under microwave radiation, reduces solvent consumption, the post-treatment is relatively simple, the yield is relatively high and no by-products exist, and can also react in the presence of a small amount of water, the reaction is easy to operate, and the method is suitable for industrial production. The method belongs to the technical field of compound synthesis.
An efficient oxidative conversion of 2-aryl-2H-chromenes to the corresponding flavones by tert-butylhydroperoxide and copper bromide
Banerjee, Dipanwita,Kayal, Utpal,Maiti, Gourhari
, p. 1667 - 1671 (2016/04/04)
A simple and efficient method has been developed for the facile oxidation of chromenes to the corresponding flavones by tert-butylhydroperoxide (TBHP) in the presence of copper(II) bromide catalyst in toluene at 80 °C in a very short time. The reaction demonstrates excellent reactivity, functional group tolerance, and good to excellent yields without using conventional strong oxidizing agents.
Synthesis of novel 4,6-diaryl-2-aminopyrimidines as potential antiplasmodial agents
Giridhar, Rajani,Tamboli, Riyaj S.,Prajapati, Dhaval G.,Soni, Sanket,Gupta, Sarita,Yadav
, p. 3309 - 3315 (2013/07/27)
A novel series of 4,6-diaryl-2-aminopyrimidines 8a-o has been synthesized and evaluated for in vitro antiplasmodial activity against Plasmodium falciparum. Out of the 15 compounds synthesized and tested, 6 compounds have shown IC50 values in the range of 1.61-9.53 μg/mL. These compounds are several times more potent than chloroquine and quinine, the two standard drugs used for the purpose of comparison.
Assessment of antiplatelet activity of 2-aminopyrimidines
Giridhar, Rajani,Tamboli, Riyaj S.,Ramajayam,Prajapati, Dhaval G.,Yadav
, p. 428 - 432 (2012/07/03)
A series of 4,6-diaryl-2-aminopyrimidines was developed as antiplatelet agents and their potency was evaluated by in vitro assay. Compound 14k was found to be two times more potent than aspirin. These encouraging results could be helpful for the development of new antiplatelet compounds.
Synthesis and preliminary biological evaluation of chrysin derivatives as potential anticancer drugs
Zheng, Xing,Zhao, Fei Fei,Liu, Yun Mei,Yao, Xu,Zheng, Zi Tong,Luo, Xing,Liao, Duan Fang
, p. 6 - 8 (2011/10/31)
A series of chrysin derivatives were prepared from 2-hydroxyacetophenone, 2,4-dihydroxyacetophenone, 2,4,6-trihydroxy- acetophenone, using modified Baker-Venkataraman transformation. Their anticancer activities in vitro were evaluated by the standard MTT method. The results of biological test showed that some of chrysin derivatives showed stronger anticancer activity than 5-fluorouracil.
A selective transformation of flavanones to 3-bromoflavones and flavones under microwave irradiation
Zhou, Zhongzhen,Zhao, Peiliang,Huang, Wei,Yang, Guangfu
, p. 63 - 67 (2007/10/03)
This paper presents the first report of a highly selective transformation of flavanones to 3-bromoflavones or flavones by microwave irradiation of the corresponding flavanone reactants and N-bromosuccinimide (NBS) in the presence of a catalytic amount of 2,2′-azobis(isobutyronitrile) (AIBN). The combination of good to excellent yields, shorter reaction time (10 min), and high levels of functional group compatibility make this an attractive synthetic approach to 3-bromoflavones and flavones.
Synthesis and inhibitory activity against COX-2 catalyzed prostaglandin production of chrysin derivatives
Dao, Tran Thanh,Chi, Yeon Sook,Kim, Jeongsoo,Kim, Hyun Pyo,Kim, Sanghee,Park, Haeil
, p. 1165 - 1167 (2007/10/03)
A series of chrysin derivatives were prepared and evaluated for their inhibitory activities of cyclooxygenase-2 catalyzed prostaglandin production. Chrysin derivatives were prepared from 2-hydroxyacetophenone, 2,4-dihydroxyacetophenone and 2,6-dihydroxyacetophenone in 2 to 4 steps, respectively. Methxoylated chrysin derivatives were converted to the corresponding hydroxylated chrysin derivatives by the reaction with BBr 3 in good yields. The inhibitory activity of the chrysin derivatives against prostaglandin production from lipopolysaccharide-treated RAW 264.7 cells was measured. We found that chrysin derivatives with 3′,4′- dichloro substituents (5e, 6e and 7e) exhibited good inhibitory activity of prostaglandin production.
CDK inhibitors having flavone structure
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, (2008/06/13)
The present invention relates to a novel flavone derivative, pharmaceutically acceptable salt, hydrate, solvate and isomer thereof which is useful as an inhibitor against Cyclin Dependent Kinase (CDK), a process for preparation thereof, and a composition of anti-cancer agent or agent for treating neurodegenerative disease comprising this compound as an active ingredient.
