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Synlett
DOI: 10.1055/a-2759-6905
Letter

Synthesis and Activity Evaluation of Gemcitabine Prodrugs with 4-(boronic acid) benzoylamide Structure

Authors

  • Chunfeng Jiang

    1   School of Biomedical and Chemical Engineering, Liaoning Institute of Science and Technology, Benxi, China (Ringgold ID: RIN117782)

  • Xianrui Wang

    1   School of Biomedical and Chemical Engineering, Liaoning Institute of Science and Technology, Benxi, China (Ringgold ID: RIN117782)

  • Changwei An

    1   School of Biomedical and Chemical Engineering, Liaoning Institute of Science and Technology, Benxi, China (Ringgold ID: RIN117782)

  • Jiaqi Jiang

    1   School of Biomedical and Chemical Engineering, Liaoning Institute of Science and Technology, Benxi, China (Ringgold ID: RIN117782)

  • Tongjia Su

    1   School of Biomedical and Chemical Engineering, Liaoning Institute of Science and Technology, Benxi, China (Ringgold ID: RIN117782)

  • Meiwei Liu

    1   School of Biomedical and Chemical Engineering, Liaoning Institute of Science and Technology, Benxi, China (Ringgold ID: RIN117782)

  • Xiaobo Xu

    2   School of Life Sciences and Biopharmaceuticals, Shenyang Pharmaceutical University, Shenyang, China (Ringgold ID: RIN58575)

  • Qinglin Zeng

    2   School of Life Sciences and Biopharmaceuticals, Shenyang Pharmaceutical University, Shenyang, China (Ringgold ID: RIN58575)

Supported by: General Project of the Education Department of Liaoning Province JYTMS20231789
Supported by: Fund of Liaoning Institute of Science and Technology 2307B14
Supported by: team of Liaoning Institute of Science and Technology XKT202304
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A convenient approach was developed for the syntheses of amide derivatives and novel Gemcitabine prodrugs with 4-(boronic acid) benzoylamide structure. The amide compounds containing phenylboronic acid structure were synthesized by a one-step reaction strategy using o-toluidine and 4-boronobenzoic acid as starting materials. And the pure product was quickly obtained through acid-base post-treatment. Moreover, the prodrugs of gemcitabine containing phenylboronic acid structure were rapidly synthesized by microchannel continuous flow technology. Three of all the obtained targets were subjected to the anti-proliferative activity test.



Publication History

Received: 26 October 2025

Accepted after revision: 29 November 2025

Accepted Manuscript online:
29 November 2025

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