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

• Main Authors: Bin Bin Huang, Ya Yi Liu, Peng Fei Zhu, Yi Cheng Jiang, Ming-An Ouyang
• Format: Article
• Language: English
• Published: MDPI AG 2020-08-01
• Series: Molecules
• Subjects: total synthesis; 5-butylpicolinic acid; natural product; alkaloid; antifungal activity
• Online Access: https://www.mdpi.com/1420-3049/25/17/3859

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.