- Nickel-catalyzed deallylation of aryl allyl ethers with hydrosilanes
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An efficient and mild catalytic deallylation method of aryl allyl ethers is developed, with commercially available Ni(COD)2 as catalyst precursor, simple substituted bipyridine as ligand and air-stable hydrosilanes. The process is compatible with a variety of functional groups and the desired phenol products can be obtained with excellent yields and selectivity. Besides, by detection or isolation of key intermediates, mechanism studies confirm that the deallylation undergoes η3-allylnickel intermediate pathway.
- Ding, Guangni,Fan, Sijie,Wang, Jingyang,Wang, Yu,Wu, Xiaoyu,Xie, Xiaomin,Yang, Liqun,Zhang, Zhaoguo
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supporting information
(2021/09/28)
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- Synthesis, molecular modelling studies of indolyl chalcone derivatives and their antimalarial activity evaluation
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Twenty one chalcone derivatives were synthesized using Claisen-Schmidt condensation, their antimalarial activity against Plasmodium falciparum was determined and quantitative structure–activity relationship (QSAR) was developed. Condensation of substituted acetophenones with various aromatic aldehydes at room temperature gave chalcones in 75–96% yield. Chalcones are secondary metabolites of terrestrial plants, precursors for the biosynthesis of flavonoids and exhibit various biological activities. Antiplasmodial IC50 (half-maximal inhibitory concentration) activity of a compound against malaria parasites in?vitro provides a good first screen for identifying the antimalarial potential of the compound. The most active compound was Trans-3-(1H-indol-3-yl)-1-(2’-hydroxyphenyl)-2-propen-1-one(1b) with IC50 of 2.1 μM/L. Molecular mechanism was explored through in silico docking & ADMET studies for the active compounds.
- Jyoti,Gaur, Rashmi,Kumar, Yogesh,Cheema, Harveer Singh,Kapkoti, Deepak Singh,Darokar, Mahendra P.,Khan, Feroz,Bhakuni, Rajendra Singh
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p. 3261 - 3268
(2019/12/11)
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- Synthesis of Polysubstituted 3-Methylisoquinolines through the 6π-Electron Cyclization/Elimination of 1-Azatrienes derived from 1,1-Dimethylhydrazine
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A convenient one pot microwave-assisted 6π-electron cyclization/aromatization approach toward 3-methylisoquinolines is reported. The starting 1-azatriene derivatives were prepared in situ by reaction of 2-propenylbenzaldehydes with 1,1-dimethylhydrazine, which exhibited superior performance when compared with other hydrazine derivatives. Minor amounts of the related 3,4-dihydro isoquinolines were formed concomitantly with the isoquinolines, and a mechanism for their generation was proposed. The reaction conditions were optimized, and its scope and limitations were explored. In general, the transformation proceeded in moderate to good yields.
- Vargas, Didier F.,Larghi, Enrique L.,Kaufman, Teodoro S.
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supporting information
p. 5605 - 5614
(2018/10/09)
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- Chemical synthesis, docking studies and biological effects of functionalized 1,3-diaryl-2-propen-1-ones on human colon cancer cells
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A series of 1, 3-diaryl-2-propen-1-ones was synthesised in order to obtain a new type of anticancer drug, designed with hybrid features to inhibit colon cancer activated receptor. Based on computational modelling and docking studies, potential inhibitors were synthesised and their biological activity evaluated. The structures of newly synthesized compounds were confirmed by1HNMR,13CNMR and Mass spectrometry. All analogues were evaluated for in vitro cytotoxicity against human colon (caco-2) cancer cell lines. Compounds 1b, 1f-1h, and 2i showed significant cytotoxicity. Chalcones 1b, 1f and 1g were identified as the most potent and selective anticancer agents with IC50 values 1 μg/mL and 1.5 μg/mL, against caco-2 cell line, respectively. In conclusion, this finding confirms the suitability of indolyl chalcone analogues as candidates for further investigation towards the management of colon cancer related diseases.
- Zhu, Guo-Min,Huang, Guo-Dong
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p. 230 - 240
(2015/09/21)
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- CARBINOL DERIVATIVES HAVING CYCLIC LINKER
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[Object] To provide a novel LXRβ agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A carbinol compound represented by the following general formula (I) or salt thereof, or their solvate.
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Page/Page column 86
(2010/03/31)
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- A new synthesis of benzofurans from phenols via claisen rearrangement and ring-closing metathesis
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Based on Claisen rearrangement, the double bond isomerization of O-allyl function together with the formation of O-vinyl function in one pot, and ring-closing metathesis (RCM), various phenols were transformed into various benzofurans in good yields.
- Tsai, Tzu-Wei,Wang, Eng-Chi,Li, Sie-Rong,Chen, Yung-Hua,Lin, Yu-Li,Wang, You-Feng,Huang, Keng-Shiang
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p. 1307 - 1318
(2007/10/03)
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