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多酚 ›› 2020, Vol. 2 ›› Issue (1): 35-42.

• • 上一篇    

A concise total synthesis of natural flavonols

Gaigai Liu 1, Shunqiang Gong 1, Zhan Li 1, Xingyi Du 1, Xiaolou Miao 2*, Xuhong Ren 1*   

  1. 1. School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China; 2. Key Laboratory of New Animal Drug Project of Gansu Province, Lanzhou Institute of Husbandry and Pharmaceutical Sciences of Chinese Academy of Agricultural Sciences, Lanzhou 730050, China
  • 出版日期:2020-12-20 发布日期:2021-01-14

A concise total synthesis of natural flavonols

Gaigai Liu 1, Shunqiang Gong 1, Zhan Li 1, Xingyi Du 1, Xiaolou Miao 2*, Xuhong Ren 1*   

  1. 1. School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China; 2. Key Laboratory of New Animal Drug Project of Gansu Province, Lanzhou Institute of Husbandry and Pharmaceutical Sciences of Chinese Academy of Agricultural Sciences, Lanzhou 730050, China
  • Online:2020-12-20 Published:2021-01-14
  • Contact: Xuhong Ren (renxuhong2008@163.com); Xiaolou Miao (miaoxiaolou@qq.com) E-mail:renxuhong2008@163.com;miaoxiaolou@qq.com

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摘要： Abstract In this study, we designed a convenient method, to total synthesis of fl avonols especially for C-5 substituted ones and derivatives on a large scale. Beginning from the inexpensively available 2,4,6-trihydroxyacetophenone through Aldol condensation reaction, I2/DMSO cyclization reaction, Oxone “one pot” oxidation, kaempferol (1) and derivative (2) was obtained in an overall yield of 35%. The structures of the target compound and key intermediates were verifi ed by MS, IR, 1 H-NMR and 13C-NMR techniques, and the structure of 5a was further confi rmed by X-ray diff raction analysis.

关键词: flavonol, I2/DMSO cyclization, oxidation

Abstract: Abstract In this study, we designed a convenient method, to total synthesis of fl avonols especially for C-5 substituted ones and derivatives on a large scale. Beginning from the inexpensively available 2,4,6-trihydroxyacetophenone through Aldol condensation reaction, I2/DMSO cyclization reaction, Oxone “one pot” oxidation, kaempferol (1) and derivative (2) was obtained in an overall yield of 35%. The structures of the target compound and key intermediates were verifi ed by MS, IR, 1 H-NMR and 13C-NMR techniques, and the structure of 5a was further confi rmed by X-ray diff raction analysis.

Key words: flavonol, I2/DMSO cyclization, oxidation

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