Improved Synthesis of Icaritin and Total Synthesis of β-Anhydroicaritin

Jie Tong; Chang Liu; Bo Wang

doi:10.1007/s40242-019-9012-x

Chemical Research in Chinese Universities ›› 2019, Vol. 35 ›› Issue (4) : 616 -620. DOI: 10.1007/s40242-019-9012-x

Article

Improved Synthesis of Icaritin and Total Synthesis of β-Anhydroicaritin

Jie Tong ¹^,²
, Chang Liu ¹^,^b
, Bo Wang ¹^,³^,^c

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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.

Keywords

Icaritin / Flavonol / Regioselectivity / Algar-Flynn-Oyamada

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Jie Tong, Chang Liu, Bo Wang. Improved Synthesis of Icaritin and Total Synthesis of β-Anhydroicaritin. Chemical Research in Chinese Universities, 2019, 35(4): 616-620 DOI:10.1007/s40242-019-9012-x

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