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    Natural products: A bridge between new targets and novel pesticide discovery
    Zhengqi FANG, Shuanhu GAO, Haibing HE
    Journal of East China Normal University(Natural Science)    2023, 2023 (1): 21-30.   DOI: 10.3969/j.issn.1000-5641.2023.01.003
    Abstract1057)   HTML48)    PDF(pc) (3235KB)(641)       Save

    Pesticides are important tools to control crop diseases and pest hazards, guaranteeing the crop harvest. Natural products and their derivatives are major sources of novel pesticides and play indispensable roles in various fields, such as insecticide, fungicide, plant growth regulation, immune regulation and so on. In recent years, numerous fields of biotechnology have made great progress, like genomics, proteomics and structural biology. And thus, the identification of pesticide targets based on natural products and the creation of novel pesticide molecules based on target structures developed rapidly. The concept, rational design, received more attention in pesticide creation. In this article, the discovery of active natural products based on existed targets or novel targets verifying by natural products were demonstrated by several cases, and the subsequent progress in the development of new pesticides were also discussed. The cases explained the important role of natural products in bridging new targets and novel pesticides.

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    Catalytic asymmetric synthesis of chiral heterocyclic compounds with CO 2 as the C1 synthon
    Zhipeng ZHAO, Ying SUN, Xiaotong GAO, Feng ZHOU
    Journal of East China Normal University(Natural Science)    2023, 2023 (1): 31-40.   DOI: 10.3969/j.issn.1000-5641.2023.01.004
    Abstract528)   HTML16)    PDF(pc) (1463KB)(635)       Save

    As the main component of greenhouse gases, CO2 represents an inexpensive and readily available renewable C1 synthon. In the past few decades, great efforts have been made toward the development of chemical processes that use CO2 as a promising fossil fuel alternative for C1 feedstocks for the production of industrially attractive chemicals. This could provide access to materials of commercial interest from an abundant, nontoxic, renewable, and low-cost carbon source, thus offering interesting opportunities for the chemical industry, organic synthesis, and so on. Considering the importance of chiral heterocycles in organic synthesis and drug development, the development of highly stereoselective and efficient catalytic asymmetric reactions using CO2 as a C1 synthon for these chiral heterocycles has received considerable attention. Successful examples for chiral lactones, carbonates, and carbamates have already been demonstrated. In this paper, we summarize the recent advances in this field.

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    Recent advances in regioselective hydrodifluoroalkylation of alkenes
    Ying ZHANG, Ling LIAO, Xiaosi HU, Jian ZHOU, Jinsheng YU
    Journal of East China Normal University(Natural Science)    2023, 2023 (1): 1-11.   DOI: 10.3969/j.issn.1000-5641.2023.01.001
    Abstract456)   HTML271)    PDF(pc) (1845KB)(359)       Save

    The regioselective hydrodifluoroalkylation of alkenes has been identified as a straightforward and highly atom-economical approach for synthesizing value-added difluoroalkylated molecules that have important applications in the pharmaceutical and agrochemical industries, as well as in the field of materials science. This is because olefins are structurally diverse raw materials that are inexpensive and easily obtainable from a wide range of sources. Recent years have witnessed significant progress in this field with the rapid development of visible-light catalysis and novel difluoroalkylating reagents. This article review summarizes the latest advances in the regioselective anti-Markovnikov and Markovnikov hydrodifluoroalkylation of various olefins, which provides an inspirational locale for researchers to engage. Herein, we supplement ideas for designing and developing new reactions, difluoroalkyl reagents, and catalytic strategies.

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    Aminocarbonylation of propylene (ethylene) epoxide over Co 2(CO) 8 catalyst modified by bidental O-containing ligand for synthesis of β-hydroxy amides
    Lin GUO, Guanghui SHI, Xiaochao CHEN, Ye LIU
    Journal of East China Normal University(Natural Science)    2023, 2023 (1): 12-20.   DOI: 10.3969/j.issn.1000-5641.2023.01.002
    Abstract347)   HTML258)    PDF(pc) (761KB)(194)       Save

    This work reports a one-step protocol for the synthesis of β-hydroxyamides via amino-carbonylation of epoxides using aromatic amines as the ammonia source instead of silylamine. The reaction was catalyzed by Co2(CO)8 modified with bidentate O-containing ligand L2, which was prepared by the oxidation of Xantphos [9,9-dimethyl-4,5-bis(diphenylphosphino)xanthene] by H2O2 as a diphosphine-dioxide. Under mild conditions (60 °C, CO 3.0 MPa, 6 h), L2-modified Co2(CO)8 efficiently catalyzed the amino-carbonylation of propylene oxide with aniline to generate 3-hydroxy-N-phenylbutanamide with the yield of 64%. The developed catalytic system exhibited fair stability and general substrate scope.

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