Benzoxazole Derivatives, Synthesis And Biological Activity Study

Recent twenty years, the research and development of fungicide industry have obtained fast development and gained the remarkable achievement. Heterocyclic compounds have characteristics like widely biological activities, low virus, efficient and friendship to environment. So it became research hotspot nowadays. Structure modification of containing benzoxazole has opened a new research area of new pesticide discovery.Benzoxazole derivatives are an important class of active compounds such as herbicides, fungicides, anticancer and preservation. The synthesis and biological activities of Benzoxazole derivatives have been a focus of considerable attention in synthetic organic chemistry as well as in medicinal chemistry, In order to find new Benzoxazole and their derivatives with high activity and low toxicily, 3-amino tyrosine ethyl ester was synthesized via a three steps synthetic sequence involving protection of amino group, nitration and reduction using L-tyrosine ethyl ester as a lead compound. It is an important medial compound. Then benzoxazole derivatives were synthesized through cyclization with the benzaldehyde or substituted benzaldehyde.The structures of all synthesized compounds were confirmed by IR, ¹H NMR, ¹³C NMR and elemental analysis. At the same time we optimized synthesis condition of the key intermediate 3-amino-L-tyrosine by shortening reactive time from 3 hours to 1.5 hours.The bactericidal activities of Partial compounds were tested, we found that some compounds have a little antibacterial activity. We have made a meaningful study for development of fungicide.