第 46 卷第 4 期 Vol. 46 No. 4 2016 年 8 月 Aug 2016

所属栏目：农药及中间体 含噻唑环核N-硝基亚胺基咪唑烷类化合物的合成及生物活性研究

钱 程1，曹 蕾1，刘 强1，邴贵芳2，方建新2，刘建兵1* （1. 湖南师范大学 石化新材料与资源精细利用国家地方联合工程实验室；化学生物学及中药分析省部共建教育部重点实验室，湖南 长沙 410081；2. 南开大学 元素有机化学研究所，天津 300071）

摘　要：以氯噻啉为先导，利用类同合成方法，保留氯噻啉结构中噻唑环2-位氯原子，通过变换噻唑环4-位取代基，设计合成了8个氯噻啉类似物。所有化合物的结构均经1H NMR、13C NMR、质谱及元素分析等确认。初步生物活性测试结果表明：该类化合物具有一定的杀虫活性。在200 μg／mL的浓度下，化合物8a和8g对桃蚜（Myzus persicae）致死率达70％。

关键词：氯噻啉类似物；生物活性；N-硝基亚胺基咪唑烷

中图分类号：TQ517　　文献标识码：A　　文章编号：1009-9212（2016）04-0013-04

Synthesis and Biological Activity of N-(Imidazolidin-2-ylidene)nitramide Containing Thiazole Moiety

QIAN Cheng1, CAO Lei1, LIU Qiang1, BING Gui-fang2, FANG Jing-xin2, LIU Jian-bing1* (1. National and Local Joint Engineering Lab for New Petro-chemical Materials and Fine Utilization of Resources, Key Laboratory of Chemical Biology and Traditional Chinese Medicine Research, Ministry of Education, Hunan Normal University, Changsha 410081, China; 2. Research Institute of Elemento-organic Chemistry, Nankai University, Tianjin 300071, China)

Abstract：Using imidaclothiz as the starting compound, eight imidaclothiz analogues were designed and synthesized according to the synthetic method of imidaclothiz where the chlorine atoms at 2-position was retained, and the 4-position was introduced with different groups. The title compounds were characterized using 1H NMR, 13C NMR, MS and elemental analysis. Preliminary bioassay results showed that the target compounds had certain insecticidal activity. At a concentration of 200 μg/mL, compound 8a and 8g showed 90% larvicidal activity against Myzus persicae 200 mg/mL.

Key words：imidaclothiz analogues; biological activity; N-(imidazolidin-2-ylidene)nitramide

作者简介：钱 程（1992-），男，湖南常德人，硕士研究生，主要从事有机合成研究（E-mail：1595764023@qq.com）。

联 系 人：刘建兵，高级工程师（E-mail：lcl6967@qq.com）。

收稿日期：2016-05-10