1-(3-氯吡啶-2-基)-5-二氟甲基-1H-4-吡唑酰胺类化合物的合成及杀菌活性  

Synthesis and fungicidal activity of 1-(3-chloropyridin-2-yl)-5difluoromethyl-1H-pyrazole-4-carboxamide derivatives

作　　者：姬文娟[1] 许天明[1] 郑志文[1] 朱冰春[1] 李姣[1] 胡伟群[1] 孔小林[1] 

机构地区：[1]浙江省化工研究院有限公司,国家南方农药创制中心浙江基地,杭州310023

出　　处：《农药学学报》2013年第4期393-397,共5页Chinese Journal of Pesticide Science

基　　金："十二五"国家科技支撑计划项目(2011BAE06B02)

摘　　要：以2,3-二氯吡啶(1)为起始原料,经肼基化、环合、水解和酰氯化反应,生成1-(3-氯-2-吡啶)-5-二氟甲基-1H-吡唑-4-甲酰氯(6),(6)与取代基苯胺(7)反应,制得13个未见文献报道的1-吡啶基吡唑酰胺类目标化合物。利用核磁共振氢谱、质谱(LC-MS)和元素分析对目标化合物的结构进行了表征。初步杀菌活性测定结果表明,在50 mg/L下,大部分目标化合物对瓜类炭疽病菌G ibberella zeae、瓜类灰霉病菌Botrytis cinerea和水稻纹枯病菌Rhizoctonia solani的抑制活性均不高,仅ZJ-10对瓜类灰霉病菌的抑制率达76.03%。1-（ 3-chloropyridin-2-yl ）-5-difluoromethyl-lH-pyrazole-4-carbonyl chloride （ 6 ） was synthesized using 2,3-dichloropyridine （ 1 ） as raw materials by hydrazinolysis, cyclization, hydrolysis, acyl chlorination. Then 13 novel title compounds were synthesized by acylation of （6） with substituted anilines（7）. The structures of the compounds were confirmed by LC-MS,1H NMR and elemental analysis. The preliminary biological activity showed that all the compounds exhibit mild inhibiting effect against all the tested strains at the concentration of 50 mg/L. Among them, the inhibitory rate of compound ZJ-10 against Botrytis cinerea was 76.03 % at the concentration of 50 mg/L.

关 键 词：1-吡啶基吡唑 吡唑甲酰胺 合成 杀菌活性 

分 类 号：O626.21[理学—有机化学]