Studies On Synthesis And Biological Activity Of Thienopyrimidine Derivatives

The derivatives of thienopyrimidine have became to be the highlight field of agrochemistry and medicine research, after being found to show widespread biological activities. However, there is little report of a generally useful synthesis of thienobispyrimidinones. In this paper, we studied the synthesis of novel thienopyrimidine derivatives and benzothienopyrimidine derivatives via aza-Wittig reaction. The condition for cyclization was researched. The spectral properties and biological activities of some compounds were also researched and some of them were found to show good herbicidal activities. What the paper studied may be summarizedas follows:1. Symmetrically or unsymmetrically 2,3,6,7-substituted thieno[2,3-d:5,4-d] dipyrimidine-4,5(3H,6H)diones were synthesized (40 Comp). The structure of most of these compounds were confirmed by 1H NMR. Some of them were confirmed by MS.2. Benzothieno[3,2-d]pyrimidin-4(3H)-dione by utilizing aza-Wittig reaction was proosed (18 Comp). The structure of all these compounds were confirmed by IR. Some of them were confirmed by 1H NMR, MS.3. The method of preparation of 2,5-diamino-3,4-(diethoxycarbonyl)thiophene was studied and the yield was improved 18% by Prolonging the reaction time and so on.4. The plant growth regulating, herbicidal activities of 32 compounds were also researched. The preliminary bioassay results showed that:most of the target compou-nds possessed not so good plant in growth regulating activities at 10 mg/L, but good herbicidal activities under test concentration. For example:5i,5v showed great inhibi-tory activity in Amaranth. At 10 mg/L, the adjusted root length inhibition rates of Ma Amaranthus retroflexus are 88.24% and 92.73%, respectively. The adjusted hypocotyl length inhibition rates of Ma Amaranthus retroflexus are 77.46% and 90.61% respectively.