Synthesis And Biologicalactivity Of Pyrazole Aryl Ketones Of HPPD Inhibitors

4-hydroxyphenylpyruvic dioxygenase(HPPD)as a protein composed by Iron and Tyrosine,could converte 4-hydroxyphenyl-pyruvate(4-HPP)into Homogentisic acid(HGA)catalytically.HGA also can produce plastoquinone and tocopherol(vitamin E)by deacidification,which are important components of biological metabolism.Therefore,some new environmental and friendly herbicides efficiently with low toxicity and residue can be developed by using HPPD inhibitors as a target with the thorough study in HPPD.91 Target compounds containing pyrazole aryl ketones were designed and synthesized as the active center of HPPD inhibitors without any reported.And the structures of these compounds were identified and confirmed by~1H NMR and MS.The biological activity of target compounds have been tested in the Southern National Pesticide Research Center of Zhejiang Base(Zhejiang Chemical Research Institute Co.,Ltd.)with reference to the"Standard Operation Procedures of Southern National Pesticide Research Center".The results showed that ZJ9268,ZJ9269,ZJ9270,ZJ9272,ZJ9277 etc.17 compounds had high herbicidal activity(80-100%)to Brassica juncea?Chenopodium serotinum and Stellaria media during common screening at 150g.a.i/ha.ZJ10348,ZJ10349,ZJ10350,ZJ10351,ZJ10354 etc.10 compounds had high herbicidal activity(80-100%)to Abutilon theophrasti?Amaranthus retroflexus?Echinochloa crusgalli and Setaria viridis during normal screening at 150 g.a.i/ha.Meanwhile,and some of the compounds were selected to study in crop safety primary research,the result showed that ZJ9286,ZJ9289,ZJ10302,ZJ10307,ZJ10308,ZJ10316 etc.6 compounds had high activity(>90%)on the Brassica juncea?Chenopodium serotinum and Stellaria media at 75 g.a.i/ha.Also,ZJ10302,ZJ10307,ZJ10308,ZJ10316 were safety to maize,rice and wheat(inhibition rate of fresh weight<10%),it could be worthy further research consequently.