杀虫剂茚虫威的合成工艺与研究.pdfVIP

杀虫剂茚虫威的合成工艺研究 摘 要 茚虫威（indoxacarb）是美国杜邦公司开发的新型噁二嗪类(oxadiazine) 杀虫剂。茚虫威是以钠通道为主要靶标，具有高效，靶向，低风险的特性。 本文综述了茚虫威的创制经纬和使用效果，概况了现有文献的合成路线。在 总结文献方法的基础上设计了一条较合理的合成路线。在实验的基础上，发现以 氯苯和 3-氯丙酸为原料，主要经过，氯化，Frieldel-Crafts酰化反应，环合， 用手性催化剂辛可宁进行手性催化反应，用 FMOC 对氨基进行保护，在碱性条件 下脱FMOC保护，得到最终产品的合成路线。 本文探讨了各步反应的机理和FMOC氨基保护和脱保护的反应条件，FMOC氨 基保护用于茚虫威全合成未见文献报道，根据核磁共振光谱确证了产品的结构。 确立了一条合成步骤少、反应条件温和、工艺稳定、适合规模化生产的合成路线。 关键词 茚虫威，手性合成，手性催化剂，FMOC保护 Abstract Indoxcarb is new insecticide invented by Dupont. It is a sodium chancel blocker insecticide with the characteristic of high activity, target selectivity and low risk. This paper describes the evolution of structure and effectiveness of usage. This paper offers the routes based on the literatures. This paper designed a reasonable route after summarizing the routes in the literaturers. According to the experimental discovery, starting from chlorination, Frieldel-Craft, cyclization to catalyzing the chiral reaction, FMOC protection。 The route is validated. This paper researched mechanism of respective reaction, including FMOC protection and relevant reaction condition， which is not found in the literature analyzed the relevant chromatography. The NMR-H validated route has advantages in terms of fewer steps, stable process that is suitable to the large scale production.