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Citation: ZHENG Hui, LIU Yun-Kui, ZHAO Qing, XU Zhen-Yuan. Synthesis and Biological Activity of Fluorine-Substituted Pyridine-Heterocyclic Carboxylate Compounds[J]. Chinese Journal of Applied Chemistry, ;2010, 27(2): 164-168. doi: 10.3724/SP.J.1095.2010.90164 shu

Synthesis and Biological Activity of Fluorine-Substituted Pyridine-Heterocyclic Carboxylate Compounds

a. Chemistry & Chemical Engineering, College of Material, Hangzhou Normal University, Hangzhou 310014;
b. College of Chemical Engineering & Materials, Zhejiang University of Technology, Hangzhou 310014

Received Date: 20 February 2009
Revised Date: 28 May 2009

In the search of bioactive compounds,a series of fluorine-substituted pyridine-heterocyclic carboxylate compounds were synthesized with methyl fluoroacetate,cyanacetamide,ethyl formic ester,alcoholic and phenolic compounds via ring closure,chlorination,hydrolyzation,acylchloriration and esterification reactions. The overall yield was about 38%. All compounds were characterized by ¹H NMR,¹³C NMR,IR,MS and elemental analysis. The preliminary bioassay results show that compounds 1e,1i,1j and 1k exhibited 61.9%~100% mortality against culex mosquito at 500 mg/L and little inhibition against several tested fungi. Compound 1k had better bioactivity and exhibited 100% mortality against armyworm and culex mosquito at 500 mg/L. The preliminary structure-activity relationship results reveal that the title phenolic compounds have good bioactivities while the alcoholic compounds do not.
- fluorinated compound,
- pyridine heterocycle,
- carboxylate,
- bioactivity
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