一类新型多取代嘌呤类化合物的合成及生物活性

以4-氯-5硝基嘧啶(3)为起始物, 经胺解、还原和环合等反应, 构建了新型的多取代嘌呤-8-硫酮(6)结构. 通过化合物6与卤代物的反应, 获得了该杂环的8位巯基衍生物7a-1~7, 7b-1~5和8, 其结构经元素分析, 1H NMR, IR及MS确证. 生物活性测试结果表明,  化合物6和7具有一定的除草和抗烟草花叶病毒活性.

Synthesis and Biological Activity of a Series of Poly-substituted Purines

Purine plays very important roles in life process,such as metabolism and heredity,while purine nucleosides and nucleotides are the key components of some important co-enzymes nucleic acids.Lots of compounds containing purine ring have been developed into drugs in treating cancer,virus infection and vascular disease.In recent years,nucleic acid chemistry is also developed into a focused field.And derivation and selective modification of purine ring have attracted great attention of researchers.Although N-benzyl adenine was found to possess a good plant growth regulation(PGR) activity and used in agriculture for a long time,there is much less attention paid on purine ring than other heterocycles in agro-chemistry field.In order to study the synthesis and biological activities of multi-substituted purines,new poly-substituted purine-8-thiones(6) were obtained from 4-chloro-5-nitropyrimidine(3) via a series of reactions as amination,reduction and cyclization.After alkylation of compounds 6,7 and 8 were obtained in high yields.The preliminary bioassay indicates that some of compounds 6,7 and 8 possess moderate herbicidal and anti-TMV activities.