Study On The Synthesis Of α-iminophophonates

α-Iminophophonates are phosphorus-containing imino functional compounds, possessing a wide range of biologic activities, such as fungicidal, herbicidal, pesticidal and so on. Their sythesis and bioactivities have attracted great attention in research. In this paper we mainly explored the synthesis of α-iminophophonates and their bioactivities. We introduced flurine atom into target compounds due to its advantage of simulation effect, electronic effect and so on. A series of α-iminophosphonates, including seven fluorine-containing, two non- fluorine-containing compounds and two N -benzoxy -α-iminophosphonates, were obtained via Michaelis-Arbuzov rearrangement reaction. This was then followed by reaction with amine, hydroxylamine hydrochloride and 2, 4-dinitrophenylhydrazine. The compounds were characterized by IR, elemental analysis and ~1H MNR spectral data. We have found two novel methods, and also optimized our reaction conditions. However, the reacion of aryl amine with acylphosphonates didn't yield the desired product. The result of bioassay indicated that the target compounds have unconspicuous antifungal activity. The experiments laid solid theoretical foundation for further research work.