New progress has been made in the construction of spiro skeleton by C-H bond activation in Dai Huixiong group, Shanghai Institute of medicine, Chinese Academy of Sciences
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Last Update: 2019-07-19
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Source: Internet
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Author: User
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Spirocyclic compounds with indole ketone skeleton widely exist in the active drug molecules, which have novel structures and wide applications, and have become the research hotspot of biomedicine The chemical synthesis of C-H bond activation strategy has the advantages of simplifying the raw materials, shortening the reaction process, realizing the rapid synthesis and modification of structural diversity molecules, and effectively overcoming the complex substrate, lengthy steps, harsh conditions, poor universality and other problems in the synthesis of spiro compounds Dai Huixiong group of Shanghai Institute of medicine, Chinese Academy of Sciences has long been committed to the exploration of new C-H bond activation reaction and its application in new drug research and development In view of the poor selectivity of C-H bond activation in the complex molecular system containing heterocycles, our group successively realized the selective activation of C-H bond by coordinating the catalyst with the guiding group Relevant research results were published in nature, J am Chem SOC., angel Chem Int ed., chem SCI., org Lett., etc Based on the above research methods, recently, a series of Rh (III) - catalyzed C-H bond activation / carbene insertion / lossen rearrangement reactions have been developed by Dai Huixiong's research group, and a kind of spiro skeleton containing indole ketone has been constructed efficiently The series reaction conditions are mild, the functional group compatibility is strong, and the substrate range is wide It can modify many drug molecules in the later stage The related results were published in angew Chem Int ed (DOI: 10.1002 / anie 201906589) The first co authors were postdoctoral Ma Biao and Shanghai University Union Peisheng Wu Peng The research work was supported by NSFC, Ministry of science and technology, Chinese Academy of Sciences, Shanghai Science and Technology Commission and other projects (source: angelw Chem Int ed.)
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