23794-73-2Relevant academic research and scientific papers
Synthesis of 4-substituted-1,2-dihydroquinolines by means of gold-catalyzed intramolecular hydroarylation reaction of n-ethoxycarbonyl-n-propargylanilines
Arcadi, Antonio,Calcaterra, Andrea,Fabrizi, Giancarlo,Fochetti, Andrea,Goggiamani, Antonella,Iazzetti, Antonia,Marrone, Federico,Marsicano, Vincenzo,Mazzoccanti, Giulia,Serraiocco, Andrea
supporting information, (2021/06/21)
An alternative Au(I)-catalyzed synthetic route to functionalized 1,2-dihydroquinolines is reported. This novel approach is based on the use of N-ethoxycarbonyl protected-Npropargylanilines as building blocks that rapidly undergo the IMHA reaction affording the 6-endo cyclization product in good to high yields. In the presence of N-ethoxycarbonyl-N-propargyl-metasubstituted anilines, the regiodivergent cyclization at the ortho-/para-position is achieved by the means of catalyst fine tuning.
Photoredox-Catalyst-Enabled para-Selective Trifluoromethylation of tert-Butyl Arylcarbamates
Chen, Yujie,Huang, Zhibin,Jiang, Yaqiqi,Li, Bao,Ma, Nana,Shi, Daqing,Shu, Sai,Yang, Shan,Zhao, Yingsheng
supporting information, p. 19030 - 19034 (2021/08/09)
The direct incorporation of a trifluoromethyl group on an aromatic ring using a radical pathway has been extensively investigated. However, the direct highly para-selective C?H trifluoromethylation of a class of arenes has not been achieved. In this study, we report a light-promoted 4,5-dichlorofluorescein (DCFS)-enabled para-selective C?H trifluoromethylation of arylcarbamates using Langlois reagent. The preliminary mechanistic study revealed that the activated organic photocatalyst coordinated with the arylcarbamate led to para-selective C?H trifluoromethylation. Ten-gram scale reaction performs well highlighting the synthetic importance of this new protocol.
Preparation method of aniline para-trifluoromethylated derivative
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Paragraph 0177-0183, (2021/08/07)
The invention discloses a preparation method of an aniline para-trifluoromethylated derivative. The method comprises the following steps: sequentially adding an aniline derivative, 4, 5-dichlorofluorescein, potassium persulfate and sodium trifluoromethanesulfinate into a glass reaction tube, and reacting at room temperature (23-25 DEG C) under 40W blue LED (light-emitting diode) by taking dimethyl sulfoxide as a solvent to obtain the aniline para-trifluoromethylated derivative. According to the invention, the aniline derivative is used as an initiator, and the raw materials are easily available and various; products obtained by the method disclosed by the invention have various types and can be directly applied to modification of drug molecules; and meanwhile, the synthesis route is safe and easy to implement, the cost is low, the reaction operation and post-treatment process are simple, the selectivity is good, the side reaction is few, and the amplification reaction can be carried out.
Identification and characterization of amino-piperidinequinolones and quinazolinones as MCHr1 antagonists
Blackburn, Christopher,LaMarche, Matthew J.,Brown, James,Che, Jennifer Lee,Cullis, Courtney A.,Lai, Sujen,Maguire, Martin,Marsilje, Thomas,Geddes, Bradley,Govek, Elizabeth,Kadambi, Vivek,Doherty, Colleen,Dayton, Brian,Brodjian, Sevan,Marsh, Kennan C.,Collins, Christine A.,Kym, Philip R.
, p. 2621 - 2627 (2007/10/03)
Several potent, functionally active MCHr1 antagonists derived from quinolin-2(1H)-ones and quinazoline-2(1H)-ones have been synthesized and evaluated. Pyridylmethyl substitution at the quinolone 1-position results in derivatives with low-nM binding potency and good selectivity with respect to hERG binding.
Synthesis and insecticidal evaluation of propesticides of benzoylphenylureas
Chen, Li,Wang, Qingmin,Huang, Runqiu,Mao, Chunhui,Shang, Jian,Bi, Fuchun
, p. 38 - 41 (2007/10/03)
Two series of benzoylphenylurea derivatives were synthesized as candidate propesticides by a nucleophilic addition reaction between 2,6-difluronbenzoyl isocyanate and N-substitutedaniline. The new compounds were identified by 1H NMR spectroscopy, electron ionization-mass spectrometry, and elemental analyses. The bioactivities of the new compounds were evaluated. All of the propesticides reported here were soluble in most organic solvents, and their hydrophobicities were improved obviously. The result of the bioactivities of the new compounds against Oriental armyworm showed that some of the new compounds are good as compared to diflubenzuron and penfluron.
