Study On Derivation And Bioactivity Of Validoxylamine A

Validamycins are safe and highly effective bio-pesticides with special modes of action. Validoxylamine A is the aglycone of the validamycin A, which exhibits a very strong competitive inhibitory activity against trehalases. Forty new compounds of validoxylamine A derivatives were prepared based on validoxylamine A as the leading compound. Their bioactivities of insecticidal, fungicidal and herbicidal activity were studied.Firstly, validoxylamine A was prepared by hydrolysis of validamycin A through the improved method of synthesis. Calcium carbonate was used as the neutralizing agent and validoxylamine A was crystallized directly from the neutralized solution. The yield of validoxylamine A was 50%. The purity was good. The process of synthesis and the separate method were simple.Three new 7'-O-chrysanthemylvalidoxylamine A were prepared in 43.3～44.3% yields by optimizing the reaction time and the molar ratio of reactants. The products were separated by twice column chromatography.7'-aldehyde validoxylamine A was prepared by the reaction of selective oxidation. The hydroxyl in the C-7' position of validoxylamine A was oxidated by active manganese dioxide under ultrasonic radiation. It was easy to operate and the yield was 77.8 %Seven new 7'-imino-validoxylamine A derivatives were synthesized by the reaction of 7'-aldehyde validoxylamine A and arylamines or alkylamines. 7'-(N-dodecylimino)validoxylamine A , which is better than the leading compound, can dissolve in organic solvent such as ethyl acetateIn the presence of p-toluenesulphonic acid, twenty-nine of acetals or ketals derivatives of validoxylamine A were prepared from validoxylamine A. The yield was about 32% by optimizing the scalar of catalyzer and the molar ratio of reactants.Preliminary method of separating validoxylamine A derivatives was found. The...