生物合成

In this paper, we studied the synthesis of novel imidazolones by utilizing aza-Wittig reaction. The spectral properties and biological activities of imidazolones were also researched and some of them were found to show good fungicidal activities.

本论文研究了应用氮杂Wittig反应，来合成新型咪唑啉酮类化合物，并探索了所合成化合物的波谱性质与生物活性，发现部分化合物具有良好的杀菌活性。

The advantages of α-hydroxyacetic acid biosynthesis over traditional chemical conversion are wide range of reaction condition,high conversion ratio and green process.

化学法生产羟基乙酸存在原料消耗大、产品收率低、环境污染严重等缺点；生物法合成羟基乙酸条件温和、底物转化率高，为绿色合成羟基乙酸提供强有力的技术支持。

New antifungal agents have been developed over the past years based on the discovery of many new target sites of Candida albicands. For example, Echinocandins, aiming at the cell wall of Candida albicands, showed strong antifungal activities to fluconazole resistant candidas and fungal biofilm. Moreover, because β-glucan synthase does not exist on the cell membrane of mammalian cells, Echinocandins has a low toxicity and a promising clinical future. Though the mechanism of Histatin is not clear, it has strong activity not only on candida resistant of polyene and azole, but also to Candida parapsilosis, Candida krusei and Cry ptococcus neoformans. Berberine and Ocimum gratissimum L. were also found to have prominent anti-fungi activities.

近年来相继提出了许多抗白念珠菌药物作用的新靶点并成功开发出一些活性强大，疗效确切的抗真菌药，如以真菌细胞壁为靶点开发出棘白菌素类药物卡泊芬净、米卡芬净等，该类药物主要抑制β-葡聚糖合成酶，体外对氟康唑耐药的念珠菌属及真菌生物被膜表现出强大的抗菌活性，又由于β-葡聚糖合成酶在哺乳类动物细胞内不存在，故具有高效低毒的临床效果，是一极具前途的新型抗真菌药；以真菌细胞膜为靶点开发出Histatin类药物，虽然作用机制目前还不完全明了，但其作用不同于临床常用的多烯类和氮唑类，并已经发现Histatin5对两性霉素B和氮唑类耐药的念珠菌有效，并且对非白念珠菌如光滑念珠菌、克柔氏念株菌、隐球菌等也有杀灭作用；通过对植物药物的研究发现黄连素和丁香罗勒Ocimum gratissimum L。

To discover new strobilurin analogues with high pesticidal activity, a series of new strobilurin derivatives containing substituted pyrazole and pyrimide ring, which included 124 novel compounds (73 compounds containing substituted pyrazole ring and 51 compounds containing substituted pyrimide ring) were designed and synthesized. In addition, 36 new intermediates were synthesized. Their structures were characterized by ~1H NMR and elemental analysis, partial compounds were characterized by MS and IR once again.

为了发现具有更好生物活性的新型Strobilurin类化合物，本论文在详尽总结文献的基础上，设计并合成了含吡唑和嘧啶环的新型Strobilurin类化合物124个，其中含吡唑环的新型Strobilurin类化合物73个，含嘧啶环的新型Strobilurin类化合物51个；未见文献报道的中间体36个，所合成的化合物经过~1H NMR、IR、LC-MS或元素分析等确定了结构。

To discover new strobilurin analogues with high pesticidal activity, a series of new strobilurin derivatives containing substituted pyrazole and pyrimide ring, which included 124 novel compounds (73 compounds containing substituted pyrazole ring and 51 compounds containing substituted pyrimide ring) were designed and synthesized. In addition, 36 new intermediates were synthesized. Their structures were characterized by 1H NMR and elemental analysis, partial compounds were characterized by MS and IR once again.

为了发现具有更好生物活性的新型Strobilurin类化合物，本论文在详尽总结文献的基础上，设计并合成了含吡唑和嘧啶环的新型Strobilurin类化合物124个，其中含吡唑环的新加热管型Strobilurin类化合物73个，含嘧啶环的新型Strob 加热管 ilurin类化合物51个；未见文献报道的中间体36个，所合成的化合物经过1H NMR、IR、LC-MS或元素分析等确定了结构。

The total synthese three natural compounds to explore enantioselective synthesis of flavanol: We use phloroglucin and 2, 4, 6-trihydroxyacetophone as starting materials to synthesis distenin in two ways; Resorcin was used to synthsis 2, 5-dimethoxymethoxyacetophone though 3 steps.

对黄烷醇化合物的立体选择性全合成进行了探索：以间苯三酚和2，4，6-三羟基苯乙酮为原料，尝试用两条路线对Distenin化合物进行了全合成研究；以对苯二酚为原料，经三步制得2，5-二甲氧甲氧基苯乙酮，与2，4，6-三甲氧甲氧基苯甲醛反应，经四步反应得到天然产物3，5，7，2′，5′-二五羟基黄烷关键中间体1-（2′，6′-二甲氧甲氧基苯）-3-（2&，4&，6-三甲氧甲氧基苯）丙烷-1R，2R-二醇83及其对映体84；简要介绍了EGCg类化合物的生物活性和研究概况。

In addition, two water-solublephosphonic acid derivatives of C〓 and two diadducts of phosphonate derivative of C〓were also prepared. All the four compounds can be dissolved in DMSO, which is asolvent easy to be soluble in water. Their DMSO aqueous solution could haveprospective applications in the field of biomedicine.

研究了富勒烯膦酸酯衍生物的水解反应，首次合成了两个水溶性富勒烯膦酸衍生物，另外还合成了两个二加成的富勒烯膦酸酯衍生物，这四个衍生物均能很好地溶解在和水互溶的DMSO中，它们的DMSO水溶液可能在生物医学研究中可能会有很好的应用价值。

Expanding pinacol reductive coupling reaction into asymmetric one with both diastereoselectivity and enantioselectivity may lead to its application in synthesising medicaments and biologic active compounds with structure of vicinal diol. Asymmetric pinacol coupling reaction is also the most compact and effecient method in synthesizing chiral ligands or chiral auxiliary with C〓 symmetry.

将这一反应发展成为既有高度的非对映选择性，又有高度对映选择性的不对称偶联反应在合成许多含有手性邻二醇结构的药物或生物活性物质将有更重要的应用，同时不对称Piancol偶联反应也是合成C〓对称性的邻二醇多用途手性配体或手性助剂的最为简捷有效的方法。

To monitor the effieciency of this site-directed serodiagnostic procedure, the synthetic peptides adhered to the microplates was biotinylated in situ with biotin of an extended spacer arm and avidin-biotinylated horseradish peroxidase complex was used.

为控制定位血清学检测质量，本研究应用长臂生物素对吸附于反应板上的合成肽作&原位&标记，经ABC结合和底物显色并计算吸附指数，首次为检测合成肽对反应板吸附性建立了一种简单可靠的方法。

Chiral 3 methy 1,4 butanediol and its derivatives are the important intermediate of synthesis of chiral smectic liquid crystal polyesters and chiral natrual products with biological activity. In the paper, a new efficient route of 3 methyl 1,4 butanediol and its two derivatives, 2 methyl 4 tetrapyranyloxy 1 butanol and 2 methyl 4 tetrapyranylbutanal, was described, and the target products were synthesized by employing asymmetric hydroboration oxidation improved.

手性2－甲基－1，4－丁二醇及其衍生物是合成各种手性近晶型液晶材料以及手性天然生物活性物质的重要中间体，以3－甲基－3－丁烯－1－醇为原料利用改进的不对称硼氢化－氧化反应，成功地合成了－2－甲基－1，4－丁二醇以及其2种手性衍生物：－2－甲基－4－四氢吡喃氧基－1－醇和－2－甲基－4－四氢吡喃氧基丁醛。

As she looked at Warrington's manly face, and dark, melancholy eyes, she had settled in her mind that he must have been the victim of an unhappy attachment.

每逢看到沃林顿那刚毅的脸，那乌黑、忧郁的眼睛，她便会相信，他一定作过不幸的爱情的受害者。

Maybe they'll disappear into a pothole.

也许他们将在壶穴里消失