Bertók Béla, Pap László, Arvai Géza, Bakonyvári Ildikó, Kuruczné Ribai Zsuzsanna
Agro-Chemie Pesticide Manufacturing Trading and Distributing Co Ltd, 1225 Budapest, Bányalég u. 2, Hungary.
Pest Manag Sci. 2003 Apr;59(4):377-92. doi: 10.1002/ps.644.
Structure-activity relationships of aryl alkynyl synergists of the general formula of Ar-Q-R, where Q represents a bridging structure, were studied using a standardised testing system and Relative Potency values. Ethers, esters, oxime ethers, amides and amines were prepared and evaluated. The length of the R-alkynyl chain, the role of the bridge and the substitution of the aromatic ring were examined systematically. The most potent compounds possessed an aromatic ring connected via a bridge of three atoms to an alkynyl chain, forming together a linear side-chain of six atoms. Several highly potent compounds were synthesised of which one (MB-599; proposed common name verbutin) was selected for development as a selective insecticide synergist in crop protection. Its high potential at practical insecticide:synergist ratios makes possible the reduction of the total amount of insect-control chemicals applied, and its use as an additive to produce new formulations of existing insecticides makes it highly advantageous in resistance management, giving a new tool to sustain the effectiveness of a wide range of insecticides. A product containing a (1+1) mixture of verbutin and beta-cypermethrin was launched in Hungary in 2002.
研究了通式为Ar-Q-R（其中Q代表桥连结构）的芳基炔基增效剂的构效关系，采用标准化测试系统和相对效价值进行研究。制备并评估了醚、酯、肟醚、酰胺和胺。系统地研究了R-炔基链的长度、桥连的作用以及芳环的取代情况。最有效的化合物具有通过三个原子的桥连连接到炔基链的芳环，共同形成一个六原子的线性侧链。合成了几种高效化合物，其中一种（MB-599；建议通用名称为verbutin）被选作作物保护中的选择性杀虫剂增效剂进行开发。其在实际杀虫剂与增效剂比例下的高潜力使得减少所施用的昆虫控制化学品总量成为可能，并且其作为添加剂用于生产现有杀虫剂的新配方使其在抗性管理方面具有高度优势，为维持多种杀虫剂的有效性提供了一种新工具。一种含有verbutin和高效氯氰菊酯（1+1）混合物的产品于2002年在匈牙利推出。
