| Nitrogen-containing benzoheterocyclic cornpounds become a focus of the research on novel pesticides for their high selection and bioactivity. On the basis of theory about drug design, such as Quantitative Structure-Activity Relationship (QSAR), two kinds of target molecular are designed. The kinds of molecular owning potential biological activity were designed, as following. They all contain sulfur atom and nitrogen atom.In order to synthesize target molecular, synthesis of five types of nitrogen-containing benzoheterocyclies has been done firstly. Compared with different synthetic methods and based on the previous researches in our laboratory, synthetic methods of these compounds were optimized. It is simple and convenient to prepare them from inexpensive and available materials. The reaction of compounds, respectively, with chloracetyl chloride occurred readily at room temperature in DMAC, to give corresponding chloracetyl-substiuted nitrogen-containing benzoheterocyclic-Purity were afforded after column chromatography or recrystallization.In the presence of potassium carbonate and TBAI in DMAC, TM1, TM2 were synthesized successfully through nucleophilic substitution reaction between N-chloroacetyl-2,4-dihydro-l,4-benzothiazine and 2-hydroxy-4,6-dimethyl pyrimidine or 2-mercapto- 4,6- dimethyl pyrimidine.Based on Bank's research, the reaction of 2,4-dihydro- 1,4-benzothiazine with 2-chloro-4,6-dimethyi pyrimidine in 10% HC1 at reflux for several hours gave 20% yield of TM3 after column chromatography.For the effect of base(K2CO3) in acetone, four types of N-chloroacetyl substituted nitrogen-containing benzoheterocycles were introduced into xazoie by the formation of thio-ether. TM4- TM7 were afforded in good yields after column chromatography or recrystallization.In conclusion, seven novel compounds with potential biological activity were synthesized by using different methods and the structure of them were identified by 1HNMR MS IR and elemental analysis.
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