Studies On Synthesis And Biological Activities Of Neonicontinoid Derivatives Containing Asymmetric Phosphorus Atom

As we know, neonicontinoid is a type of high effect activity and low toxicity insecticide, and these insecticides are in great demand at present, and are manufactured all over the word. The 3-(aminomethyl)pyridine is proved to be an important active group in those neonicotiniod insecticides, and the two nitrogen atom of the active group combine with nicotine acetylcholine receptor (nAchR)of insecticide and inhibit the normal nervous cells conduction with fatal effects, So, more and more attentions are focused in novel nicotine insecticides and their analogyIn order to search novel neonicontiniod insecticides, we designed and synthesized 15 novel title compounds, starting from natural chiral aminoalcohol and 3-pyridine aldehyde Their structures were confirmed by IR ¹HNM ³¹PNMR MS and Elemental Analysis. The properties of physical chemical and spectroscopy of these compounds were systematically investigated. The synthetic methods and reaction condition were also studied. The molecular formula of the title compounds can be shown as following respectively.(1)2-Thio-2-(3-pyridylmethylamino)-3-benzyl-4-methoxycarbonyl-1,3,2-oxazaphosph olidines(2)0-alkyl(α-hydroxy)methyl-3-pyridylphenylphosphinate R=i-tutyl,t-butyl,n-tutyl,i-propyl,n-Propyl, ethyl, Methyl,bromoethylThe results of preliminary bioassay show the target compounds possess pesticidal and herbicide activities to some extent.