4,5,5-三氟-N-(杂芳基甲基)戊-4-烯酰胺的合成及杀线虫活性

植物寄生线虫可能对全球农作物造成严重的危害。本研究设计合成了15个未见文献报道的4,5,5-三氟戊-4-烯酰胺衍生物,并测定了它们的离体活性和在沙土中的活体杀线虫活性,且进一步研究了沙土活体活性较好的化合物在基质中的活体杀线虫活性。离体测试结果表明:部分目标化合物表现出较好的杀线虫活性,其中含呋喃环的化合物B 8对南方根结线虫Meloidogyne incognita和松材线虫Bursaphelenchus xylophilus均表现出优异的杀线虫活性,LC50/72 h值分别为1.22 mg/L和0.53 mg/L。此外,在沙土活体活性测试中,大部分化合物在40 mg/L时对南方根结线虫具有100%的抑制作用,其中含苯并噻唑环的化合物B10的活性最好,在2.5 mg/L时抑制率为66.0%。在基质中的活体活性测试结果表明,含噻吩环的化合物B6活性最好,在5 mg/L时对南方根结线虫的抑制率为31.0%。初步的构效关系分析显示,含无取代五元环如噻吩、呋喃和噻唑的化合物的活性优于含大体积的六元环或稠环的化合物。

Challenges and risks associated with impurity profiles in technical grade crop protection products produced semi-synthetically from natural products

The safety of crop protection products and their safe use is of paramount importance and requires that crop protection products are consistently marketed and used worldwide in the required registered quality.To meet these high-quality requirements,the highest demands must be placed on the production and purification of technical-grade crop protection products.In this context,impurity profiles are of utmost importance,as unknown impurities at higher than registered concentrations may pose new unknown toxicological risks to users,consumers,and the environment.Particularly high demands are placed on the production and purification of technical grade semisynthetic derivatives of fermentatively derived natural products to meet the required regulatory specifications,to ensure that relevant impurities do not exceed maximum allowable concentrations,to ensure the safe use of such products,and to eliminate any unknown product safety risks.The challenges associated with the manufacture and purification of Afidopyropen and the product safety risks associated with various qualities of technical grade Emamectin benzoate are discussed in detail.