Practical Synthesis of α‐Amyrin, β‐Amyrin, and Lupeol: The Potential Natural Inhibitors of Human Oxidosqualene Cyclase

A practical synthesis of α‐amyrin (1), β‐amyrin (2), and lupeol (3) was accomplished in total yields of 32, 42, and 40% starting from easily available ursolic acid (4), oleanolic acid (5), and betulin (6), respectively. Remarkably, these three natural pentacyclic triterpenes exhibited potential inhi...

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Veröffentlicht in:Archiv der Pharmazie (Weinheim) 2017-12, Vol.350 (12), p.n/a
Hauptverfasser: Chen, Dongyin, Xu, Fengguo, Zhang, Pu, Deng, Jie, Sun, Hongbin, Wen, Xiaoan, Liu, Jun
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Sprache:eng
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Zusammenfassung:A practical synthesis of α‐amyrin (1), β‐amyrin (2), and lupeol (3) was accomplished in total yields of 32, 42, and 40% starting from easily available ursolic acid (4), oleanolic acid (5), and betulin (6), respectively. Remarkably, these three natural pentacyclic triterpenes exhibited potential inhibitory activity against human oxidosqualene cyclase. A practical synthesis of α‐amyrin (1), β‐amyrin (2), and lupeol (3) was accomplished in total yields of 32, 42, and 40% starting from easily available ursolic acid, oleanolic acid, and botulin, respectively. These three natural pentacyclic triterpenes exhibited potential inhibitory activity against human oxidosqualene cyclase.
ISSN:0365-6233
1521-4184
DOI:10.1002/ardp.201700178