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| 含P_H键苯并磷杂环化合物与醛反应的研究 | |
| 引用本文： | 黄君珉,陈茹玉. 含P_H键苯并磷杂环化合物与醛反应的研究[J]. 高等学校化学学报, 2000, 21(10): 1510-1514 |
| 作者姓名： | 黄君珉 陈茹玉 |
| 作者单位： | 南开大学元素有机化学研究所, 元素有机化学国家重点实验室, 天津 300071 |
| 基金项目： | 国家自然科学基金! (批准号 :2 9972 0 2 1)资助 |
| 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A2羟基膦酸衍生化喹唑啉酮含磷类似物2或Ò,并研究了含P_C_O结构的2或Ò转化为含P_O_C结构的3或Ó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. |
| 关 键 词： | 喹唑啉酮含磷类似物 重排反应 非对映异构现象 生物活性 |
| 文章编号： | 0251-0790(2000)10-1510-05 |
| 收稿时间： | 1999-11-05 |
Studies of Quinazolone Analogues Containing Phosphorus and Their Reaction with Aldehydes |
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| HUANG Jun-Min,CHEN Ru-Yu. Studies of Quinazolone Analogues Containing Phosphorus and Their Reaction with Aldehydes[J]. Chemical Research In Chinese Universities, 2000, 21(10): 1510-1514 | |
| Authors: | HUANG Jun-Min CHEN Ru-Yu |
| Affiliation: | Institute of Elemento organic Chemistry, National Laboratory of Elemento organic Chemistry, Nankai University, Tianjin 300071, China |
| 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. |
| Keywords: | Quinazolone analogues containing phosphorus Diastereoisomerism Rearrangement reaction Biological activity |
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