苯甲酰基甲磺酰胺的合成与杀菌活性

李兴海; 祁之秋; 钟昌继; 张扬; 纪明山; 王道全

苯甲酰基甲磺酰胺的合成与杀菌活性

1.
沈阳农业大学植物保护学院,沈阳 110161
2.
连云港中化化学品有限公司,江苏连云港 222500
3.
中国农业大学理学院应用化学系,北京 100193

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出版历程
- 收稿日期: 2008-04-10

The Synthesis and Fungicidal Activity of Benzoyl Methanesulfonamides

1.
Plant Protection College,Shenyang Agricultural University,Shenyang 110161,China
2.
Sinochem LianyungangChemicals Co. ,Ltd. ,Lianyungang 222500,Jiangsu Province,China
3.
Department of AppliedChemistry,China Agricultural University,Beijing 100193,China

摘要

摘要: 以苯乙酮为原料,用三氧化硫·二氧六环进行磺化,经碱中和后制备得到苯甲酰甲磺酸盐;与草酰氯在DMF为催化剂的条件下反应生成磺酰氯,再与胺反应,制备得到14个苯甲酰基甲磺酰胺,其中13个为新化合物。其结构通过1H NMR、IR和元素分析确证。在50 μg/mL浓度时,该系列化合物对番茄灰霉病菌Botrytis cinerea、小麦赤霉病菌Gibberlla zeae、水稻纹枯病菌Rhizoctonia solani、梨黑星病菌Venturia nashicola菌丝生长均具有很好的抑制活性,其中化合物 B-8、B-9、B-10、B-12 对番茄灰霉病菌的EC50值分别为1.0、0.2、1.2、0.4 μg/mL,接近或优于对照药剂嘧霉胺, B-8、B-10、B-11 对小麦赤霉病菌的EC50值分别为0.07、0.2、0.05 μg/mL,优于对照药剂多菌灵。
- 苯乙酮 /
- 苯甲酰基甲磺酰胺 /
- 合成 /
- 杀菌活性
Abstract: A series of benzoyl methanesulfonamides have been synthesized.They were obtained by sulfonation,chlorization,amination from the readily available acetophenone.Their structures were confirmed by 1H NMR,IR and elementary analysis.The bioassay indicated that some of them possess certain fungicidal activity against Botrytis cinerea,Gibberlla zeae,Rhizoctonia solani,Venturia nashicola at a dose of 50 μg/mL.The EC50 value of title compounds B-8、B-9、B-10、B-12 was reached 1.0,0.2,1.2 and 0.4 μg/mL against B.cinerea,the effect was approximated or better than pyrimethail and EC50 value of title compounds B-8、B-10、B-11 was reached 0.07,0.2 and 0.05 μg/mL against G.zeae,the effect was better than carbendazim.
- acetophenone /
- benzoyl methanesulfonamides /
- synthesis /
- fungicidal activity

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