Search | Engineering

订阅投稿

首页工程期刊工程焦点工程成就工程前沿关于我们 English

资源类型

期刊论文 2

年份

2022 1

2020 1

关键词

分子对接 1

合成 1

杀线虫活性 1

杀菌活性 1

检索范围：

排序：展示方式：

Continuous deacylation of amides in a high-temperature and high-pressure microreactor

《化学科学与工程前沿（英文）》 2022年第16卷第12期页码 1818-1825 doi: 10.1007/s11705-022-2182-y

摘要： The deacylation of amides, which is widely employed in the pharmaceutical industry, is not a fast reaction under normal conditions. To intensify this reaction, a high-temperature and high-pressure continuous microreaction technology was developed, whose space-time yield was 49.4 times that of traditional batch reactions. Using the deacylation of acetanilide as a model reaction, the effects of the temperature, pressure, reaction time, molar ratio of reactants, and water composition on acetanilide conversion were carefully studied. Based on the rapid heating and cooling capabilities, the kinetics of acetanilide deacylation at high temperatures were investigated to determine the orders of reactants and activation energy. This microreaction technology was further applied to a variety of other amides to understand the influence of substituents and steric hindrance on the deacylation reaction.

关键词： amide deacylation microreactor flow chemistry reaction intensification

HTML PDF 收藏

含硫醚和砜亚结构的新型芳香酰胺类衍生物的设计、合成及生物活性 Article

华学文, 刘南南, 周沙, 张蕾蕾, 殷昊, 王桂清, 范志金, 马翼

《工程（英文）》 2020年第6卷第5期页码 553-559 doi: 10.1016/j.eng.2019.09.011

摘要：

近年来，土壤线虫危害日趋严重，然而市场上应用的杀线虫剂品种匮乏且结构单一。氟吡菌酰胺（fluopyram）是德国拜耳公司开发的琥珀酸脱氢酶抑制剂（SDHI）类杀菌剂，因其高效和作用机制新颖被广泛用于土壤线虫的防治。本文以杀菌、杀线虫剂氟吡菌酰胺为分子骨架，通过引入硫醚和砜亚结构，设计合成了两个系列的结构新颖的目标化合物，并经核磁共振氢谱（¹H NMR）、核磁共振碳谱（¹³C NMR）和高分辨质谱（HRMS）表征新结构。经生物活性测试发现，与对照药氟吡菌酰胺相比，大多数目标化合物在200 μg·mL⁻¹浓度下显示出优异的杀线虫活性，而当浓度降低为100 μg·mL⁻¹时，线虫死亡率大大降低，其中，化合物I-11、II-6除外。在杀菌活性方面，化合物I-9具有优异的抑菌率，其分子对接结果将为高活性杀菌先导化合物的设计和探索提供重要的理论指导。

关键词：合成杀线虫活性杀菌活性分子对接