Agricultural chemicals with multifunctional applications in crop protection have attracted increasing attention.Herein,two new series of thiazole and imidazo[1,2-a]pyridine derivatives containing a hydrazone substruct...Agricultural chemicals with multifunctional applications in crop protection have attracted increasing attention.Herein,two new series of thiazole and imidazo[1,2-a]pyridine derivatives containing a hydrazone substructure were designed and synthesized via a concise synthesis route.Bioassay results showed that most of the thiazole derivatives exhibited broad-spectrum fungistatic activities,which were exemplified by compounds 1c,1e,1g,1h and 1j.In particular,compound 1e displayed excellent in vitro inhibitory effects with the EC50 values of 5.00,18.24,6.94,and 3.03μg/mL against the fungi Botrytis cinerea,Cytospora sp,Fusarium graminearum,and Fusarium solani,respectively.Detached fruit experiments against tomato gray mold(caused by B.cinerea)in vivo revealed that the control efficiency of compound 1e at 10,20 and 40μg/mL for 5 days was 35.05%,54.14%and 81.83%,respectively,which was comparable and even superior to that of the fungicide carbendazim.Additionally,the title compounds also showed remarkable larvicidal activity against M.separata and some compounds exhibited good aphicidal activity.In a word,the bioassay indicated that a certain number of title compounds had multiple biological activities.Given their excellent antifungal and larvicidal characteristics,these interesting derivatives based on the title compounds could be served as new scaffolds for the development of pesticide with multifunctional applications.展开更多
We herein report two crystals based on 2-（imidazo[1,2-a]pyridin-2-yl）-2-oxoacetic acid rad- ical and its perchlorate, and investigate the relationship between magnetic properties and crystal stacking structures or s...We herein report two crystals based on 2-（imidazo[1,2-a]pyridin-2-yl）-2-oxoacetic acid rad- ical and its perchlorate, and investigate the relationship between magnetic properties and crystal stacking structures or supramolecular interactions. 2-（imidazo[1,2-a]pyridin-2-yl）- 2-oxoaeetic acid radical in two crystals mainly exist as diamagnetic dimer formed via short atomic contacts or supramolecular interactions （hydrogen bonds, anion-Tr or lone- pair-~r interactions）, leading to low magnetic susceptibilities. 2-（imidazo[1,2-a]pyridin-2-yl）- 2-oxoaeetic acid radical crystal exhibits quasi-one-dimensional columnar stacking chain and weak antiferromagnetism. However, its perchlorate crystal possesses one-dimensional double- stranded chain structure assembled through double hydrogen bonds and anion-To interactions, and reveals weak ferromagnetism.展开更多
以聚乙二醇400(PEG-400)作溶剂,通过CuSO4/KI催化的邻氨基吡啶与苯乙酮的串联式缩合-环化-芳构化反应,发展出一种高效且环境友好型的合成2-苯基咪唑并[1,2-a]吡啶的方法.该方法具有操作简单、使用无毒性PEG-400作反应介质、催化剂安全...以聚乙二醇400(PEG-400)作溶剂,通过CuSO4/KI催化的邻氨基吡啶与苯乙酮的串联式缩合-环化-芳构化反应,发展出一种高效且环境友好型的合成2-苯基咪唑并[1,2-a]吡啶的方法.该方法具有操作简单、使用无毒性PEG-400作反应介质、催化剂安全价廉等优点.所有产物结构经1 H NMR及13 C NMR进行了确认.展开更多
基金supported by the National Natural Science Foundation of China(31972303)the Natural Science Basic Research Program of Shaanxi Province(Program No.2023-JC-YB-144,2023-JC-YB-719).
文摘Agricultural chemicals with multifunctional applications in crop protection have attracted increasing attention.Herein,two new series of thiazole and imidazo[1,2-a]pyridine derivatives containing a hydrazone substructure were designed and synthesized via a concise synthesis route.Bioassay results showed that most of the thiazole derivatives exhibited broad-spectrum fungistatic activities,which were exemplified by compounds 1c,1e,1g,1h and 1j.In particular,compound 1e displayed excellent in vitro inhibitory effects with the EC50 values of 5.00,18.24,6.94,and 3.03μg/mL against the fungi Botrytis cinerea,Cytospora sp,Fusarium graminearum,and Fusarium solani,respectively.Detached fruit experiments against tomato gray mold(caused by B.cinerea)in vivo revealed that the control efficiency of compound 1e at 10,20 and 40μg/mL for 5 days was 35.05%,54.14%and 81.83%,respectively,which was comparable and even superior to that of the fungicide carbendazim.Additionally,the title compounds also showed remarkable larvicidal activity against M.separata and some compounds exhibited good aphicidal activity.In a word,the bioassay indicated that a certain number of title compounds had multiple biological activities.Given their excellent antifungal and larvicidal characteristics,these interesting derivatives based on the title compounds could be served as new scaffolds for the development of pesticide with multifunctional applications.
基金This work was supported by the National Natural Science Foundation of China （No.21172210）.
文摘We herein report two crystals based on 2-（imidazo[1,2-a]pyridin-2-yl）-2-oxoacetic acid rad- ical and its perchlorate, and investigate the relationship between magnetic properties and crystal stacking structures or supramolecular interactions. 2-（imidazo[1,2-a]pyridin-2-yl）- 2-oxoaeetic acid radical in two crystals mainly exist as diamagnetic dimer formed via short atomic contacts or supramolecular interactions （hydrogen bonds, anion-Tr or lone- pair-~r interactions）, leading to low magnetic susceptibilities. 2-（imidazo[1,2-a]pyridin-2-yl）- 2-oxoaeetic acid radical crystal exhibits quasi-one-dimensional columnar stacking chain and weak antiferromagnetism. However, its perchlorate crystal possesses one-dimensional double- stranded chain structure assembled through double hydrogen bonds and anion-To interactions, and reveals weak ferromagnetism.
文摘以聚乙二醇400(PEG-400)作溶剂,通过CuSO4/KI催化的邻氨基吡啶与苯乙酮的串联式缩合-环化-芳构化反应,发展出一种高效且环境友好型的合成2-苯基咪唑并[1,2-a]吡啶的方法.该方法具有操作简单、使用无毒性PEG-400作反应介质、催化剂安全价廉等优点.所有产物结构经1 H NMR及13 C NMR进行了确认.
