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Synthesis of Novel Spinosyn A Analogues by Pd-Mediated Transformations

机译:通过Pd介导的转化合成新型Spinosyn A类似物

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摘要

The concept of modern crop protection demands for a continuous supply of new or modified established pesticides to avoid the development of serious resistances. Recent reports on the insecticidal spinosyns 1 and 2 show that also this class of pest managing agents is increasingly exposed to theformation of resistances. The synthesis of new derivatives is therefore highly desirable. We describe in this paper aconvergent approach towards novel enantiopure spinosyn A analogues of type 3, which is based on investigations of structure-activity relationships and employs a twofold Heck reaction as key step for the preparation of the tricyclic backbone assembly.
机译:现代农作物保护的概念要求不断供应新的或改良的既定农药,以避免产生严重的抗药性。关于杀虫多杀菌素1和2的最新报道表明,这类害虫处理剂也越来越受到抗药性的影响。因此,非常需要合成新的衍生物。我们在本文中描述了一种针对新型3型对映体纯多杀菌素A类似物的融合方法,该方法基于对结构-活性关系的研究,并采用双重Heck反应作为制备三环骨架组装的关键步骤。

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