Design, Synthesis, Structure, and Acaricidal/Insecticidal Activity of Novel Spirocyclic Tetronic Acid Derivatives Containing an Oxalyl Moiety
作者:Zhihui Liu、Qiong Lei、Yongqiang Li、Lixia Xiong、Haibin Song、Qingmin Wang
DOI:10.1021/jf203722z
日期:2011.12.14
1.4- and 2.3-fold as high as the activities of commercial Spiromesifen, respectively, against spider mite eggs. Moreover, most of the target compounds exhibited insecticidalactivities against Lepidoptera pest. Interestingly, compounds containing alkylamino-substituted oxalyl moiety showed obvious selectivity between spider mite larvae and eggs because the activities against spider mite eggs of 7g and
通过关键中间体3-(2,4,6-三甲基)-2-oxo-1-oxaspiro [4.4] -decyl-3-en-4设计并合成了一系列含有草酰部分的新型螺环四酸衍生物-ol。通过1 H NMR和元素分析或高分辨率质谱(HRMS)鉴定目标化合物。生物测定的结果表明,大多数目标化合物对胭脂红蜘蛛幼虫和卵具有出色的杀螨活性。特别是二异丙基氨基草酰化合物7g和哌啶草酰化合物7h分别是市售Spiromesifen对红蜘蛛卵的活性的1.4倍和2.3倍。而且,大多数目标化合物对鳞翅目害虫表现出杀虫活性。有趣的是,含有烷基氨基取代的草酰部分的化合物在红蜘蛛幼虫和卵之间显示出明显的选择性,因为对7g和7h的红蜘蛛卵的活性是对红蜘蛛幼虫的25倍,而Spiromesifen在这些活性上没有显着差异。这意味着将草酰部分引入螺环四氢苯甲酸可能会导致新的生物活性特征。
Benzylamine derivative
申请人:Nagasawa Masaaki
公开号:US20060194841A1
公开(公告)日:2006-08-31
The invention provides a compound which exhibits satisfactory peroral absorbability and excellent antagonistic activity against NK-1 receptor or NK-2 receptor. The compound is a benzylamine derivative represented by formula (1) or a salt thereof.
The invention provides a compound which exhibits satisfactory peroral absorbability and excellent antagonistic activity against NK-1 receptor or NK-2 receptor. The compound is a benzylamine derivative represented by formula (1) or a salt thereof.