Progresses in research of α-Oxophosphonic acid derivatives, including the synthesis and biological activities of thirteen series compounds are summarized. In order to obtain higher herbicidally active new phosphonate derivative with commercial potential. One approach to design a inhibitor of pyruvate dehydrogenase with a novel structure by using biochemical reasoning was attempted. The study of structure- activity relationship and then optimizing the structure by chemical modification were carried out on the basis of the study of synthesis, mechanism, biochemistry and biological activities test. α- (Substituted phenoxy acetoxy) alkyl phosphonates with good herbicidal activities and plant growth regulating activities as lead compound have been founded and demonstrated as a kind of inhibitors of pyruvate dehydrogenase complex.

Key words: BIOLOGICAL ACTIVITY, OXOPROPENOIC ACID P, DEHYDROGENASE, INHIBITOR, PLANT GROWTH REGULATORS, HERBICIDES, PHOSPHONIC ACID ESTER