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以取代苯酚、多聚甲醛和取代苯胺为原料,在无催化剂的条件下,通过Mannich缩合反应合成了一系列新型3,6(8)-二取代-2,4-二氢-1,3-苯并!嗪类化合物。结果表明,取代苯酚和取代苯胺的取代基为供电子基时,合成产物的产率高于吸电子取代基的。产物的结构用1H NMR、13C NMR、IR和MS等进行了表征。初步测试了目标化合物的杀菌活性,部分化合物具有较好的杀菌活性。当浓度为25 mg/L时,化合物4j和4d对菌核病菌的抑制率分别为86.1%和81.5%,化合物4i对灰霉病菌的抑制率为81.6%。
A series of novel 3,6 (8) -disubstituted-2,4-dihydro-1,3-dihydro-1,3-benzodiazepines were synthesized by Mannich condensation reaction using substituted phenols, paraformaldehyde and substituted anilines as raw materials. Benzoxazines. The results show that when the substituents of substituted phenols and substituted anilines are electron donating groups, the yield of synthesized products is higher than that of electron - withdrawing substituents. The structure of the product was characterized by 1H NMR, 13C NMR, IR and MS. The bactericidal activity of the target compounds was preliminary tested, and some of the compounds showed good bactericidal activity. When the concentration was 25 mg / L, the inhibitory rates of compounds 4j and 4d against Sclerotinia sclerotiorum were 86.1% and 81.5%, respectively, and that of compound 4i against Botrytis cinerea was 81.6%.