| Anticoagulant rodenticides are a kind of good palatability, efficient, safe rodenticides, since80s are widely used in China’s pastoral areas and the city anti-rat. With the use of anticoagulant rodenticides increase of years, the resisrance gradually increased. To improve the existing anticoagulants effects, a variety of new research on the anticoagulant rodenticide has important practical significance.In this paper, we design two new anticoagulant rodenticides A and B with4-hydroxy-coumarin. We also proposed the theory to increase the acute toxicity and resolve the resistance problem by adding fluoride to the existing anticoagulant rodenticides.Firstly, the synthesis of1-bromo-2-fluoroethane based on the raw materials of2-chloroethanol. We use4-bromoaniline and cinnamic acid as original material to synthesize4-biphenyl bromide, cinnamoyl chloride and4-bromine-4’-cinnamoylbiphenyl. Then, making use of these intermediates, we can synthesize A, B. Besides, the optimum methods were also confirmed.Then, the structure of all the inmediates, such as4-biphenyl bromide, cinnamoyl chloride, and4-bromine-4’-cinnamoyl biphenyl were demonstrated by IR and other means. Besides, we also test and verificate the synthesis routes of various immediates to find the opitimal reaction conditions. Finally, by the test of IR,1H NMR, melting point determination, and other pthysical and chemical methods, we conculded that the target product-novel anticoagulant rodenticides A and B were synthesized.Lastly, both the acute orally toxicity and the Palatability of the desired product A and B were tested in the no-choice and choice experiments. Our statistics demonstrate that the introduction of fluoride acetyl into the bromine position of the bromodialone leads to an enormous increase in the acute toxicity. The novel compounds A and B have both merits of acute and chronic rodenticides, and their acute toxicity increases gradually with the decrease of the group connected to fluoride acetyl. |
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