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以蒽醌为原料,经Schmidt重排为5,6-二氢-二苯并[b,e]氮杂-6,11-二酮,再经氯磺酰化和胺化合成了一系列新颖的2-(烃基胺磺酰基)-5,6-二氢-二苯并[b,e]氮杂-6,11-二酮.结构经1H NMR,13C NMR和高分辨质谱确证.初步的生测结果表明,它们对棉花立枯病菌、油菜菌核病菌和芦笋茎枯病菌具有一定的杀菌活性.其中,2-(3-三氟甲基-4-溴苯基胺磺酰基)-5,6-二氢-二苯并[b,e]氮杂-6,11二酮(4u)对芦笋茎枯病菌有良好的杀菌活性,在50μg/m L浓度下抑制率达96.3%,与对照药剂百菌清基本相当(在50μg/m L浓度下的抑制率为98.8%).初步的构效关系分析指出,氟原子的引入有利于杀菌活性的提高.
Anthraquinone as raw material, rearranged by Schmidt to 5,6-dihydro-dibenz [b, e] azepine-6,11-dione, and then chlorosulfonated and aminated to a series of Novel 2- (hydrocarbylsulfamoyl) -5,6-dihydro-dibenz [b, e] azepine-6,11-dione The structure was confirmed by 1H NMR, 13C NMR and high resolution mass spectrometry. The results of preliminary bioassay showed that they had certain bactericidal activities against Rhizoctonia solani, Sclerotinia sclerotiorum and Asparagus stem borer.Among them, 2- (3-trifluoromethyl-4-bromophenylaminosulfonyl) -5,6-dihydro-dibenzo [b, e] azepine-6,11 dione (4u) had good bactericidal activity against Asparagus officinalis, with the inhibition rate of 96.3 at the concentration of 50μg / mL %, Which was almost equivalent to chlorothalbuterol (98.8% inhibition at 50μg / mL) .A preliminary analysis of the structure-activity relationship indicated that the introduction of fluorine atom was beneficial to the increase of bactericidal activity.