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Multistep Synthesis and Nematicidal Activity of 2-(8-azabicyclo[3.2.1]octan-3-yl)-3-imino-2,3-dihydro-1 H -isoindol-1-One Derivatives
Chemistry of Heterocyclic Compounds ( IF 1.4 ) Pub Date : 2021-02-05 , DOI: 10.1007/s10593-021-02864-z
Jun Xu , Tianjiao Yang , Jiayi Wang , Gonghua Song

Novel 2-(8-azabicyclo[3.2.1]octan-3-yl)-3-imino-2,3-dihydro-1H-isoindol-1-ones derived from 5-HT3 receptor antagonists hexahydroazepinylbenzamides were designed and synthesized through isocyanide insertion reaction. All target compounds were evaluated against pinewood nematodes B. xylophilus and root-knot nematodes M. incognita. Good lethal rate (75%) for 3-(tert-butylimino)-5-chloro-2-(8-methyl-8-azabicyclo[3.2.1]octan-3-yl)-2,3-dihydro-1H-isoindol-1-one and serious nervous curl effect against pinewood nematodes B. xylophilus for 3-(tert-butylimino)-2-(8-methyl-8-azabicyclo[3.2.1]octan-3-yl)-2,3-dihydro-1H-isoindol-1-one were observed at 10 mg/l. The inhibition activities of 3-[(4-methoxyphenyl)imino]-2-(8-methyl-8-azabicyclo[3.2.1]octan-3-yl)-2,3-dihydro-1H-isoindol-1-one against root-knot nematodes M. incognita were 84% at 160 mg/l and 60% at 20 mg/l for in vitro test and test tube test, respectively.



中文翻译:

2-(8-氮杂双环[3.2.1]辛烷-3-基)-3-亚氨基-2,3-二氢-1 H-异吲哚-1-酮衍生物的多步合成及杀线虫活性

设计并合成了由5-HT3受体拮抗剂六氢hydro庚啶基苯甲酰胺衍生的新型2-(8-氮杂双环[3.2.1]辛烷-3-基)-3-亚氨基-2,3-二氢-1 H-异吲哚-1-酮异氰酸酯插入反应。对所有目标化合物针对松材线虫B. xylophilus和根结线虫M进行了评估。隐身。3-(丁基亚氨基)-5-氯-2-(8-甲基-8-氮杂双环[3.2.1]辛烷-3-基)-2,3-二氢-1 H的致死率(75%)-isoindol-1-one对3-(丁基亚氨基)-2-(8-甲基-8-氮杂双环[3.2.1] octan-3-yl)-2的松材线虫B. xylophilus具有严重的神经卷曲作用, 3-二氢-1 H观察到10 mg / l的-isoindol-1-one。3-[(4-甲氧基苯基)亚氨基] -2-(8-甲基-8-氮杂双环[3.2.1]辛-3-基)-2,3-二氢-1 H-异吲哚-1-醇的抑制活性一个对根结线虫中号在体外试验和试管试验中,分别为160 mg / l和84%在20 mg / l时的隐身

更新日期:2021-02-05
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