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Improved Synthesis of Icaritin and Total Synthesis of β-Anhydroicaritin

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Chemical Research in Chinese Universities Aims and scope

Abstract

Natural products icaritin and β-anhydroicaritin with P-glycoprotein(P-gp) inhibitory activities were efficiently synthesized in nine steps from commercially available phloroglucinol. A modified Algar-Flynn-Oyamada cyc-lization and relay Claisen-Cope rearrangement were employed in this concise route. Our synthesis offers opportunities to synthesize various icariin analogues for biological and pharmacological investigations.

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Authors and Affiliations

  1. CAS Key Laboratory of High-performance Synthetic Rubber and Its Composite Materials, Key Laboratory of Green Chemistry and Process of Jilin Province, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, 130022, P. R. China

    Jie Tong, Chang Liu & Bo Wang

  2. University of Chinese Academy of Sciences, Beijing, 100049, P. R. China

    Jie Tong

  3. University of Science and Technology of China, Hefei, 230026, P. R. China

    Bo Wang

Authors
  1. Jie Tong
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  2. Chang Liu
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  3. Bo Wang
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Corresponding authors

Correspondence to Chang Liu or Bo Wang.

Additional information

Supported by the National Natural Science Foundation of China(No.21672203).

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Tong, J., Liu, C. & Wang, B. Improved Synthesis of Icaritin and Total Synthesis of β-Anhydroicaritin. Chem. Res. Chin. Univ. 35, 616–620 (2019). https://doi.org/10.1007/s40242-019-9012-x

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  • DOI: https://doi.org/10.1007/s40242-019-9012-x

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