氨基甲酸-2-氯吡啶-5-甲酯化合物的合成与抑菌活性  

Synthesis and fungicidal activity of(2-chloropyridin-5-yl)methyl carbamates

作　　者：刘长春[1] 

机构地区：[1]江苏食品药品职业技术学院医药与健康管理学院,江苏淮安223003

出　　处：《农药学学报》2015年第1期97-100,共4页Chinese Journal of Pesticide Science

摘　　要：以芳香硝基化合物、2-氯-5-吡啶甲醇和一氧化碳为原料,在Pd-Fe/Ti O2催化下进行羰基化反应,合成了11个新型氨基甲酸-2-氯吡啶-5-甲酯化合物,其结构经1H NM R和M S表征。初步抑菌活性测定结果表明:在50 mg/L下,大多数目标化合物对4种供试病原菌具有一定的抑制活性,其中化合物3f(4-甲氧基苯基氨基甲酸-2-氯吡啶-5-甲酯、3h(2,4-二氯苯基氨基甲酸-2-氯吡啶-5-甲酯)和3j(3,4-二氯苯基氨基甲酸-2-氯吡啶-5-甲酯)对小麦赤霉病菌Gibberella zeae的抑制率达77.3%以上,3f对苹果轮纹病菌Physalospora piricola的抑制率达82.5%,与对照药多菌灵接近;所有化合物在50 mg/L下对番茄灰霉病菌Botrytis cinerea的抑制活性均优于对照药多菌灵。Eleven novel （2-chloropyridin-5-yl）methyl carbamates were synthesized by Pd-Fe/TiO2 catalyzed carbonylation of aromatic nitro-compounds and （2-chloropyridin-5-yl）methanol with carbon monoxide. Their structures were confirmed by ^1H NMR and MS. Preliminary fungicidal activity tests indicated that some of the target compounds exhibited certain degree of inhibiting effect against four tested strains at the concentration of 50 mg/L. The inhibition rate against Gibberella zeae was over 77.3% for compound 3f [ （ 2-chloropyridin-5-yl ） methyl （ 4-methoxyphenyl ） carbamate ], 3h [ 2- chloropyridin-5 -yl ） methyl （ 2,4 -dichlorophenyl ） carbamate ~ and 3j [ （ 2-chloropyridin-5 -yl ） methyl （ 3, 4-dichlorophenyl） carbamate]. Compound 3f showed 82.5% of inhibition rate against Physalospora piricola, that was almost equal to carbendazim. All compounds showed better fungicidal activities against Botrytis cinerea than carbendazim.

关 键 词：氨基甲酸酯 2-氯-5-甲基吡啶 羰基化 抑菌活性 

分 类 号：O623.626[理学—有机化学] S482.2[理学—化学]