- Optimization of diarylpentadienones as chemotherapeutics for prostate cancer
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Our earlier studies indicate that (1E,4E)-1,5-bis(1-alkyl-1H-imidazol-2-yl)penta-1,4-diene-3-ones and (1E,4E)-1,5-bis(1-alkyl-1H-benzo[d]imidazol-2-yl)penta-1,4-diene-3-ones exhibit up to 121-fold greater antiproliferative potency than curcumin in human p
- Patanapongpibul, Manee,Zhang, Changde,Chen, Guanglin,Guo, Shanchun,Zhang, Qiang,Zheng, Shilong,Wang, Guangdi,Chen, Qiao-Hong
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p. 4751 - 4760
(2018/08/21)
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- A waste-minimized protocol for copper-catalyzed Ullmann-type reaction in a biomass derived furfuryl alcohol/water azeotrope
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We report the use of biomass-derived furfuryl alcohol as an effective bidentate ligand able to promote the Ullmann-type copper-catalyzed coupling of aryl halides with heteroaromatic or aliphatic amines. Furfuryl alcohol (FA) can be mixed with water to form the corresponding azeotrope (20 wt% of FA) and therefore can be easily recovered and reused. This protocol is efficiently applied to substrates with various electronic nature and affords the expected products (27 examples) in generally good to excellent yields. It has also been demonstrated that the protocol is both chemically and environmentally effective as the azeotropic mixture can be easily and almost quantitatively recovered at the end of the process.
- Ferlin, Francesco,Trombettoni, Valeria,Luciani, Lorenzo,Fusi, Soliver,Piermatti, Oriana,Santoro, Stefano,Vaccaro, Luigi
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supporting information
p. 1634 - 1639
(2018/04/12)
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- A N - aryl pyrazole compounds and N - aryl imidazole compound of preparation method
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The invention discloses a preparation method of an N-arylpyrazole compound and an N-arylimidazole compound. The method comprises the following steps: reacting at 20-120 DEG C for 6-48 hours by taking aryl halide and pyrazole or imidazole as substrates and copper salt as a catalyst in an organic solvent in the presence of alkali and a nitrogenous ligand under nitrogen protection; and after the reaction is finished, separating and purifying a reaction liquid to obtain the N-arylpyrazole compound or the N-arylimidazole compound. A product prepared by utilizing the method disclosed by the invention can not only be directly used, but also be used for other reactions as a substrate and has the advantages of moderation in adopted reaction condition, simple operation step and post-processing process, high yield and suitability for large-scale production.
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Paragraph 0120; 0121; 0122; 0123; 0124; 0125
(2017/10/05)
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- Structure activity relationships in reactivators of organophosphorus inhibited acetylcholinesterase. VII. 1 Aryl 2 hydroxyiminomethyl 3 methylimidazolium iodides
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A series of 1 aryl 2 hydroxyiminomethyl 3 methylimidazolium iodides, where the aryl group is either phenyl or substituted phenyl, was prepared and tested for their reactivating potency on phosphorylated acetylcholinesterase (AChE) and for anti AChE activity. The in vitro testing revealed that some of the new compounds are good reactivators. Correlations between their structure and biological activities have been attempted.
- Franchetti,Grifantini,Martelli,Stein
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p. 18 - 22,21,22
(2007/10/05)
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