Chemical Research in Chinese Universities

, Volume 35, Issue 4, pp 616–620 | Cite as

Improved Synthesis of Icaritin and Total Synthesis of β-Anhydroicaritin

  • Jie Tong
  • Chang LiuEmail author
  • Bo WangEmail author


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.


Icaritin Flavonol Regioselectivity Algar-Flynn-Oyamada 


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Supplementary material

40242_2019_9012_MOESM1_ESM.pdf (1.6 mb)
Improved Synthesis of Icaritin andTotal Synthesis of β-Anhydroicaritin


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Copyright information

© Jilin University, The Editorial Department of Chemical Research in Chinese Universities and Springer-Verlag GmbH 2019

Authors and Affiliations

  1. 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 ChemistryChinese Academy of SciencesChangchunP. R. China
  2. 2.University of Chinese Academy of SciencesBeijingP. R. China
  3. 3.University of Science and Technology of ChinaHefeiP. R. China

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