以双炔酰菌胺为模板,利用“基团反转”原理将酰胺中的羰基和氮原子交换位置,设计了一系列苯乙酰儿茶酚胺类化合物.从取代苯乙酮出发,经过溴代、胺化、还原制备2-氨基-1-取代苯乙醇(6),然后与取代苯乙酸反应制备酰胺(7),最后经烷基化得到一系列保持氮原子位置不变的N-(2-烷氧基-2-取代苯基乙基)苯乙酰胺类化合物(8).所有目标化合物均通过核磁共振氢谱、元素分析或高分辨质谱确认,并测试了其生物活性.结果表明,部分化合物对黄瓜霜霉病具有较好的防治活性,化合物8k在浓度为100 μg/mL时对黄瓜霜霉防效可达75％.研究还发现,该类化合物均对蚜虫具有较好的防治效果.%Mandipropanid is the first mandelamlamide fungicide on the market. A series of novel N-(2-alkoxy-2-substituted phenyl-ethyl) phenyl amide(8) was designed according to exchange the position of NH and C = 0 from mandipropamid. The target compounds were synthesized from benzene acetic acid and aceto-phenone(3) by bromination, animation and so on. Their structures were characterized by 'H NMR, elemental analysis or high resolution mass spectra(HRMS). The results of the preliminary biological activity tests show that some of them like compound 8k exhibit good anti-fungal activities against Pseudoperonospora cubenis at 100 μg/mL. The study also finds that these compounds have a certain control on the effect of Tetranychus cinnaba-rinus.
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