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KMID : 0903519980410060471
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Journal of the Korean Society of Agricultural Chemistry and Biotechnology
1998 Volume.41 No. 6 p.471 ~ p.476
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A Synthesis of New 2-Iminothiazolines and Their Antifungal Activities(2)
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조광연/Cho, Kwang Yun
한호규/남기달/최경자/Hahn, Hoh Gyu/Nam, Kee Dal/Choi, Gyung Ja
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Abstract
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A synthesis and the screening of new 2-iminothiazolines (IV) of which structures are modified based on a lead compound, thiazoline for development of new agrochemical fungicide were described. Bromination of acetoacetanilides (I) which were prepared by the reaction of diketene with anilines gave the corresponding γ-bromoacetoactanilide (II). Treatment of II with N-phenyl-N´-methyl thiourea (III) afforded IV, structure of which was confirmed by various spectroscopic methods. Antifungal activity of the new IV was tested against six kinds of typical plant diseases (in vivo). The IV with aromatic substituents showed remarkable activity against the Pyricuraria oryzae at 250 ppm in primary screening. The candidates with control value over 90% in primary screening were selected and further tested for second screening at lower concentrations. The IV which has an electron-withdrawing substituent such as halogen, especially fluorine in aryl group showed a higher activity as compared to those with electron-donating group and meta substituent was for optimal position.
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KEYWORD
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