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    Home > Xu Tao Group of Ocean University of China has made new progress in the construction of diaryl substituted active molecular skeleton catalyzed by chiral phosphine

    Xu Tao Group of Ocean University of China has made new progress in the construction of diaryl substituted active molecular skeleton catalyzed by chiral phosphine

    • Last Update: 2019-05-29
    • Source: Internet
    • Author: User
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    Recently, the international well-known journal organic letters published the latest research results of Professor Xu Tao's research group, School of medicine, Ocean University of China -- using TERT phosphine to catalyze the construction of polysubstituted benzofuran structure with dienyl ester and p-methylquinonone olefin, and using it in the total synthesis of active natural products The article title is "highly regio - and enantioselective" Dienylation of p-Quinone Methides Enabled by Organocatalyzed Isomerization/Addition Cascade of Allenoates” ( DOI: 10.1021/acs.orglett.9b01110)。 1,1 '- diaryl substituted chiral compounds are widely found in active natural products and drug molecules, such as candidate drug molecule cdp840 (PDE4 inhibitor), drug molecule r-tolterodine, drug molecule chlorpheniramine, etc all have 1,1' - diaryl substituted structures and chiral center compounds On the basis of previous research, Associate Professor Wang De of Xu Tao's research group (chem SCI., 2015, 6, 7319; Chem EUR J., 2014, 20, 15325), using p-quinone alkene (p-qms) as starting material, under the action of r-sitcp -The 1,1 '- diaryl substituted conjugated diene structure was constructed by QMS and 1,6-conjugated addition / aromatization in one step The reaction conditions are mild, the substrate has high universality and functional group compatibility, which meets the requirements of atomic economy The substrate has a wide range of applicability and more than 30 different substituents are compatible The group also studied the mechanism of the reaction, proposed the possible intermediates of the reaction and verified them by deuterium experiment and other control experiments In the later stage of this work, the derivative synthesis and methodology research of guiding active drug molecules are in-depth progress The activity screening of some of these compounds initially shows that they have strong cytotoxicity to a variety of cancer cells (the IC 50 value of MKN-45 half lethal rate of gastric cancer cells reaches 2.2 mm water level, and the IC 50 value of other common human cancer cells respectively in 2.2-7.2 mm), the activity test results provide a strong support for the subsequent structural modification This part of the work has been supported and helped by Professor Yang Jinbo and Professor Wang Xin, and the relevant activity research is in the process of design The first completion unit of this paper is the school of medicine of Ocean University of China The co correspondents are Wang De, associate professor, young experts of Taishan Scholars, outstanding young scholars of Aoshan talents, Xu Tao, Professor of Ocean University of China, song Zefeng and Wang Weijia, graduate students of School of medicine Also participated in part of the research work of this paper At the same time, the work was supported by the National Natural Science Foundation of China Youth Fund, NSFC Shandong joint fund key projects and the launch fund of "Young Talents Program" of Ocean University of China.
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