Discovery Of Pyrimidine Benzylamine Diphenyl Ether Leads And Mechanistic Study On A Novel LiAlH₄-promoted Reductive Rearrangement Of Benzamide Derivatives Via Neighboring-pyrimidine Participation

Chapter 1,It is reported that pyrimidine compounds have various biological activity. The herbicides basing on pyrimidines have been paid great attention to. In recent years ,there are many new herbicides. Benzylamine compounds have special structure and strong herbicidal activity.We have found that pyrimidinylbenzylamine compounds have special structures and strong herbicidal activity. To design and synthesis is our major goal.Chapter 2, pyrimidine benzylamine diphenyl ether leads have been designed, synthesised and tested the herbicidal activity.The pyrimidine and diphenyl ether are the basic copose cells. Fifteen compounds leads have been synthesized and tested by HNMR , IR and the herbicidal activity against barnyard grass, hairy fingers were tested . The compounds of 25, 70, 71 and 73 have strong herbicidal activity against hardy cereal plant (avena sativa) weeds and 9 class of suppression ratio against barnyard grass, hairy fingers. Herbicidal activity is relevant to the aryl substituents. So we have found the herbicidal activity have a connection with structures.Chapter 3,six-substituented pyrimidinylbenzylamine compounds have been designed and intermediate compound 76 have been synthesised by using improvement means. By a lot of experiments, FeCl₂.4H₂O and NH₄Cl as catalyst mixture and methanol/water as solvent is favorable for reduction.Chapter 4, the reduction of benzamide derivatives of neighboring-pyrimidine by Lithium aluminium hydride to amine . The reaction is out of the way .So we are interesting in searching after the mechanism on a Novel LiAlH4-promoted Reductive Rearrangement of Benzamide Derivatives Via Neighboring-pyrimidine Participation by changing in their receiver structures, Labling by the LiAlD₄, intermolecular and intramolecularnucleophilic substitutions and monocrystal structureet al. At last a possible mechanism is proposed.It is very interesting to exploit the new organic paths.