Concise Total Synthesis and Antifungal Activities of Fusaric Acid, a Natural Product

  • Molecules. 2020 Aug 25;25(17):3859. doi: 10.3390/molecules25173859.
Bin Bin Huang  1 Ya Yi Liu  1 Peng Fei Zhu  1 Yi Cheng Jiang  1 Ming-An Ouyang  1
Affiliations
  • 1. Key Laboratory of Biopesticide and Chemical Biology (Ministry of Education), Fujian Agriculture and Forestry University, Fuzhou 350002, China.
Abstract

The total synthesis of a natural product alkaloid fusaric acid (FA), which exhibits Herbicide, fungicide, Insecticide and even diverse notable pharmacological activities, was accomplished in four steps using commercially available Materials. The synthesis, based on a unified and flexible strategy using 6-bromonicotinaldehyde as a common intermediate, is concise, convergent, practical and can be carried out on a two-gram scale. This approach could be readily applicable to the synthesis of its analogues. In addition, FA had a wide range of inhibitory activities against 14 plant pathogenic fungi in this study, which demonstrated that as a leading compound, and it has great potential to be further developed as an agricultural fungicide.

Keywords
5-butylpicolinic acid; alkaloid; antifungal activity; natural product; total synthesis.
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