CAJ | 학술논문

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.
이용함P-H건분병린잡배화합물여철적반응，설계합성료신적α-간기련산연생화규서람동함린유사물2혹Ⅱ，병연구료함P-C-O결구적2혹Ⅱ전화위함P－O－C결구적3혹Ⅲ적중배반응，목표화합물적결구경NMR，IR，MS화원소분석증실.결합NMR수거，탐토료화합물2인구유C*화P*량개수성중심이산생적비대영이구현상급기경보특정.대소합성적화합물진행료초보생물활성측시，발현부분화합물구유흔호적항식물병원진균(평과반점락협병균)작용화일정적인체포진병독억제활성.
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.