The Synthesis Of Strobilurin Fungicides

Strobilurins are agricultural fungicides which contain (E)-β-methoxyacrylate subunit or similar structural unit. So far, some of these fungicides have been commercialized. Studies on the mode of action of strobilurins revealed that these compounds inhibit the respiration chain of fungi, and their wide application prospects make it very important to design and synthesize similar compounds with more biological activity.In this paper, we focused our attention on molecular design of strobilurins and their synthetic research, highly stereoselective reactions (Claisen condensa-tion and O-methylation reaction) were selected to synthesize pharmacophore.The present thesis falls into four chapters. In the first chapter, structure-activity relationships of strobilurins and their synthetic methods were introduced, which can be used to direct our research on strobilurins. In the second chapter, we adopted the so-called "side chain first, pharmacophore second" method to synthesize strobilurins having two pharmacophores. Subsequently, we optimized the synthetic routes. Nevertheless, activity tests showed that the designed compound needs further modification. In the third chapter, thiophene side chain were firstly synthesized, then based on the result obtained on chapter two, strobilurins having one pharmacophore were synthesized. It reveals that the so-called "pharmacophore first, side chain second" method dose not have synthetic feasibility. In the last chapter, we summarized our research on strobilurins. All of these works gives value to further research.