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功能化的6-芳基水杨酸片段广泛地存在于各种天然产物以及活性分子中.在基于杂草抗性的分子设计中,6-芳基取代的水杨酸衍生物作为反抗性乙酰羟酸合成酶抑制剂的关键药效团发挥着至关重要的作用.在前期工作中,探索了两种策略可以合成6-芳基取代水杨酸片段,但不能有效地实现在6-芳基水杨酸片段母核结构中的底物多样化.因此,通过微波辅助的Suzuki偶联反应,成功合成了多取代的6-芳基水杨酸片段.这一方法具有反应时间短、反应收率高等优点,并且实现了底物多样化,为后期合成具有反抗性乙酰羟酸合成酶抑制剂奠定了基础.
Functionalized 6-aryl salicylic acid fragments are widely present in a variety of natural products as well as active molecules.In the design of weed resistance-based molecules, 6-aryl substituted salicylic acid derivatives act as reactive acetyls The key pharmacophore of hydroxyacid synthetase inhibitors play a crucial role.In the previous work, we explored two strategies to synthesize 6-aryl substituted salicylic acid fragments, but can not effectively achieve the 6-aryl Substrates in the core-shell structure of the base-salicylic acid fragments were diversified.Thus, polysubstituted 6-aryl-salicylic acid fragments were successfully synthesized by microwave-assisted Suzuki coupling reaction.This method has the advantages of short reaction time, High yield, and achieve the diversification of substrates, lays the foundation for the later synthesis of a reactive acetohydroxy acid synthase inhibitor.