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【答案】应助回帖
 商家已经主动声明此回帖可能含有宣传内容
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小老婆: 金币+25, 翻译EPI+1, ★★★很有帮助, 感觉不是很正宗，有点谷歌翻译的感觉，可能比我自己翻译的还差点，不过还是非常感谢啊。 2016-04-19 21:15:56
中间体10 是 目标化合物 11a-k的 关键中间体，其有 两种合成 方法。方法一（Scheme 1）：根据文献[10-11]，从 中间体6 直接合成 中间体10，以 中间体7、中间体3 和 甲醇钠 为 初始原料，以 乙二醇乙醚 为催化剂，以 正庚烷 为溶剂，加热回流 反应，且 需要分水器。方法二（Scheme 2）：即 本文的 合成方法。方法一 虽然从 中间体7 直接 合成中间体10，但 收率低、纯度低、原料难溶于 正庚烷、需要 加热回流 且 需要 分水器 操作繁琐。方法二虽然 比方法一 多出三步，但收率高，纯度高，总体收率 高于 方法一 且 反应条件温和，操作简单方便，是较好的 合成中间体10的 方法，因此 本文采用 方法二 合成中间体10。
Regarding key intermediate 10 of target compound 11a-k, there are 2 synthetic schemes. Scheme 1: according to reference [10-11], intermediate 10 can be directly synthesized from intermediate 6, wherein intermediate 7, 3 and sodium methoxide act as initial raw materials, glycol ether acts as catalyst, n-heptane is selected as solvent, in addition, heating reflux and water knockout drum are needed. Scheme 2: also the proposed scheme in this paper. Although by scheme 1, intermediate 10 can be directly synthesized from inter mediate 7, the yield and purity are low, raw materials are hard to be dissolved by n-heptane, operations are complex as heating reflux and water knockout drum are needed. On the contrast, although scheme 2 has 3 more procedures than scheme 1, it is still a better scheme for its advantages including higher yield, purity, and overall yield, milder reaction condition, simpler operation. Therefore, this paper adopts scheme 2 to synthesize intermediate 10.
生物活性 测定结果 表明, 化合物结构 对 杀蚜虫活性 有 显著影响, 其中 R2基团 对 活性的影响最大, 当R1 都是 -CH3时，R2 为B时, 活性最高，LC50 为3.45mg/L（化合物11c)；R2为A、D或G时时, 化合物活性 有所降低，但依然 表现出 较优的 杀蚜虫活性；R2为 C、E或F时，化合物 杀蚜虫活性 明显下降。总体来说, 活性数据 大小顺序为C＞D＞G＞C＞E＞F。E/Z 异构体 对 化合物的活性 也有一定影响，对比11a（E体）和11b（Z体），11h（Z体）和11i（E体），Z异构体的 活性 略优于 E异构体的 活性。
The measurement results of bioactivity show that compound structure is of significant influence to aphicide activity, wherein R2 group has the largest influence. When R1 is -CH3, R2 is B, the aphicide has the highest activity, LC50 is 3.45mg/L（compound 11c); When R2 is A, D or G, compound activity is decreased in certain degree, but still remain good aphicide activity; When R2 is A,D or F, aphicide activity is significantly reduced. Generally speaking, the activity data are in follow order: C＞D＞G＞C＞E＞F. In addition, E/Z isomer is of certain influence to compound activity. By comparing 11a（E structure） and 11b（Z structure）, 11h（Z structure） and 11i（E structure）, it can be known that Z isomer has slightly higher activity than that of E isomer. |
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