期刊论文

An Efficient Synthesis of Functionalized 6-Arylsubstituted Salicylates via Microwave Irradiation

Yang Guangfu

英文

有机化学

0253-2786

2017

37

5

1266-1272

10.6023/cjoc201612049

(201203022):公益性行业(农业)科研专项经费 (2014BAD23B01):国家科技攻关计划 (No.21372093):国家自然科学基金 (201203022):Project supported by the Special Fund for Agroscientific Research in the Public Interest (2014BAD23B01):the National Key Technologies R&D Program (21372093):the National Natural Science Foundation of China

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Functionalized 6-arylsalicylate substructures occur in a variety of pharmacologically relevant natural products and bioactive compounds. Especially 6-arylsubstituted salicylates, as a key pharmacophore of anti-resistant acetohydroxyacid synthase (AHAS) inhibitors have played a lead role in combatting the weed-resistance issues. Previously, we have explored two new methods to synthesize position-6 aryl substituted salicylic acid fragment. However, these two methods failed to introduce various substituents into salicylic acid. Here an efficient method for the synthesis of 6-substituted salicylat...

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.