【作者】 解正峰；

【导师】 曹玲华；

【作者基本信息】 新疆大学 ， 有机化学， 2003， 硕士

【摘要】 磷酰三胺类化合物具有优良的杀菌、抗病毒作用，其中部分还有抗肿瘤活性。硫脲类化合物有很好的杀菌和抗甲状腺活性等生理作用；硫脲的糖基衍生物也有很强的生理活性，同时它又是一种重要的有机合成中间体。国内曾有报道，利用磷酰二氨基异硫氰酸酯与胺反应合成磷酰三胺，但有关磷酰二氨基肼与糖基异硫氰酸酯反应的研究还未见报道。我们利用磷酰二氨基肼与糖基异硫氰酸酯反应，设计并合成了一系列同时含有磷酰三胺、糖基和硫脲基片段的新化合物共42个：N-芳基（烷基）-N′-芳基（烷基）-N″-（乙酰化糖基硫代亚脲基）磷酰三胺（21个）和N-芳基（烷基）-N′-芳基（烷基）-N″-（糖基硫代亚脲基）磷酰三胺（21个）。 本论文的主要工作是： 1．通过POCl₃的胺解、肼解等反应，制备磷酰二氨基肼； 2．利用亲核加成反应，制备N-芳基（烷基）-N′-芳基（烷基）-N″-（乙酰化糖基硫代亚脲基）磷酰三胺； 3．用糖的脱乙酰化反应制备N-芳基（烷基）-N′-芳基（烷基）-N″-（糖基硫代亚脲基）磷酰三胺。 所有新化合物的结构均经IR、¹H NMR、³¹P NMR、MS、元素分析进行确证。文中并对代表性化合物的质谱裂解做了诠释。更多还原

【Abstract】 Phosphorotriamides have strong antibacterial activity and antiviral action, but parts of them have antitumorial activity. Ureas and thioureas not only have strong antibacterial activity, but also have other bioactivities such as antithyroid activity etc. Glycosyl derivatives of thiourea have many strong biological activities. It also is versatile reagent in organic synthesis. There were some reports about preparation the phosphorotriamides through the reaction of phosphorodiamidic isocycanates with amine. There are no reports on the study about the reaction of phosphorodiamidohydrazides with glycosylisothiocycanates. We designed and synthesized a series new compound, which contain the fragments of phosphorotiamide, glycosyl and thioureylene. We have synthesized 42 compounds, they are the derivatives of N-Aryl (Alkyl)-N’ -Aryl (Alkyl)-N" -(Acetylglycosyl thioureylene) Phosphoric triamides and N-Aryl (Alkyl)-N’ -Aryl (Alkyl)-N" -(Glycosyl thioureylene) Phosphoric triamides.The major work of the thesis:1. The preparation of phosphorodiamidohydrazides through animation and hydrazinolysis reaction.2. Preparation the N-Aryl (Alkyl)-N’ -Aryl (Alkyl)-N" -(acetylGlycosyl thioureylene) phosphoric Triamides using the nuclephilic addition reaction.3. Preparation the N-Aryl (Alkyl)-N ’ -Aryl (Alkyl)-N " -(Glycosyl thioureylene) Phosphoric triamides by the action of deacetylation of suger.Their structures were confirmed by IR, ’H NMR, 31P NMR , MS spectral data and elemental analysis. The mass spectrums of some representative compounds were explained in detail.更多还原