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含P-H键苯并磷杂环化合物与醛反应的研究
Studies of Quinazolone Analogues Containing Phosphorus and Their Reaction with Aldehydes
【摘要】 利用含P_H键苯并磷杂环化合物与醛的反应 ,设计合成了新的α 羟基膦酸衍生化喹唑啉酮含磷类似物 2或Ⅱ ,并研究了含P_C_O结构的 2或Ⅱ转化为含P_O_C结构的 3或Ⅲ的重排反应 ,目标化合物的结构经NMR ,IR ,MS和元素分析证实 .结合NMR数据 ,探讨了化合物 2因具有C 和P 两个手性中心而产生的非对映异构现象及其氢谱特征 .对所合成的化合物进行了初步生物活性测试 ,发现部分化合物具有很好的抗植物病原真菌 (苹果斑点落叶病菌 )作用和一定的人体疱疹病毒抑制活性
【Abstract】 A series of 1 methoxycarbonylmethyl 2 (1 substituted hydroxymethyl) 3 benzyl 2,4 dioxo 1,3,2 benzodiazaphosphorins 2 or Ⅱ and their rearrangement reaction products 3 or Ⅲ have been synthesized by the reaction of aldehydes and P_H reagent. Their structures were confirmed by elemental analysis, NMR, IR and MS. On the basis of NMR analyses, we studied the diastereoisomerism phenomenon of the products 2 or Ⅱ and the rearrangement reaction by which the products 3 or Ⅲ were formed. The results of preliminary bioassay show that some of the target compounds have good in vitro activity against HSV 1 and (or) excellent fungicidal activity. [WT5HZ]
【Key words】 Quinazolone analogues containing phosphorus; Diastereoisomerism; Rearrangement reaction; Biological activity;
- 【文献出处】 高等学校化学学报 ,Chemical Research In Chinese Universities , 编辑部邮箱 ,2000年10期
- 【分类号】O626
- 【被引频次】2
- 【下载频次】164