氨化合物

The direct incorporation of U-13C glucose was estimated by the intensity increase of m/z to F(F was parent fragment, and n was the carbon number in the fragment), while the total isotope incorporation from the added 13C could be calculated according to the abundance ratio increment summation from m/z (Fa+1) through (Fa was the fragment containing all original skeleton carbons, and T was the carbon number in the amino acid molecule). The 13C enrichment in the target compound was expressed as atom percentage excess, and that of D-amino acid needed to be corrected by the coefficient of hydrolysis-induced racemization. The 13C enrichment reflected the carbon turnover velocity of individual amino acid enantiomers, and was powerful to investigate the dynamics of soil amino acids.

外加葡萄糖直接合成氨基酸的比例可利用质谱碎片的相对强度变化来评价（n为质谱碎片F中含有的碳原子数目）；而源于葡萄糖的13C同位素在氨基酸分子中的富集程度是所有同位素峰相对强度变化的总和。13C在目标化合物中的富集比例用原子百分超评价，D氨－基酸的APE还需进一步利用水解诱导的外消旋化系数校正。13C在目标化合物中的富集程度可反映各氨基酸手性异构体的碳循环速率大小，是研究土壤氨基酸动态变化的有力工具。

Then Doripenem came into the market in the July ,2005. We studied the synthesis of Doripemen.Firstly, we synthesized the chemical 2 from the starting material------o-hydroxylphenylacylamine through Reformastky reaction, alkylation, Diekmann reaction, enolization, esterification and etc. Secondly, we synthesized the chemical 3 from L — hydroxylproline through the protection of carboxyl, amidogen and hydroxyl group, reduction by NaBr, SN_2 substitution and Mitsumobu reaction.

我们以水杨酰胺为起始原料，经Reformatsky反应、烷基化、Diekmann环合、烯醇化、酯化等反应合成双环母核2；再从L-羟基脯氨酸出发，经酯化保护羧基、保护氨基、保护羟基、硼氢化还原酯得醇、Sn2取代和Mitsumobu反应等合成巯基侧链3；最后由化合物3经脱保护、水解得硫醇，和化合物2在二异丙基乙基胺的作用下缩合，最后Pd／C催化脱保护，历经16步反应最终得到产物多尼培南。

Nitrogen heterocyclics ; Oxygen heterocyclics ; Cobalt ; Ammine complexes

氮杂环化合物；氧杂环化合物；钴；氨络合物

Based on the previous literatures, the following major innovation works were carried out in this dissertation:(1) The derivatization reaction conditions of ephedrine and pseudoephedrine with sensitive derivation reagent in aqueous system were studied and two new methods were developed for the assay of them by microemulsion electrokinetic chromatography and micellar electrokinetic chromatography with LIF detection. The sensitivity and analysis times were greatly improved compared with the previous reports;(2) A new method of CZE with indirect LIF detection was developed for the simultaneous determination of six coumarin compounds (esculin, esculetin, isofraxidin, genistein, naringin and sophoricoside) with fluorescein as the probe. The proposed method enlarges the application range of LIF detector, and provides new approach for the analysis of certain compounds difficult to derivatize;(3) Based on the above research, an MEKC with indirect LIF detection method for the simultaneous determination of adenine and guanine in DNA extracts from fungus, maize and soybean was established;(4) A new method for the investigation of the complexes formed between human serum albumin and ampicillin sodium under the simulated physiology conditions using laser light scattering technique was developed.

该论文在综述前人工作的基础上，开展了如下未见文献报道的创新性的研究工作：(1)使用灵敏的衍生试剂对麻黄碱和伪麻黄碱在水体系中的衍生反应条件进行了系统研究，建立了微乳电动色谱-激光诱导荧光检测法和胶束电动色谱—激光诱导荧光检测法测定麻黄碱和伪麻黄碱的灵敏分析新方法，与以前的报道相比，灵敏度和分析时间均有很大改善；(2)使用荧光素钠作为背景荧光试剂，建立了同时分析测定六种黄酮类化合物(秦皮甲素、秦皮乙素、异秦皮定、染料木素、柚皮苷和槐角苷)的毛细管区带电泳—间接激光诱导荧光检测新方法，扩大了激光诱导荧光检测的应用范围，对难衍生化合物的分离分析提供了一种新思路和新途径；(3)以荧光素钠作为背景荧光试剂，建立了一种用于同时测定食品提取DNA中的腺嘌呤和鸟嘌呤含量的胶束电动色谱—间接激光诱导荧光检测新方法；(4)用动态和静态激光散射法研究了模拟生理条件下人血清白蛋白与氨比西林钠盐相互作用所形成的复合物，为药物分子与蛋白质的相互作用、药代动力学等的研究提供了一种新思路。

Methods: In this paper, a quinazoline purine analogues for the parent nucleus, respectively, and four of its seven introduced to replace the structure of diverse and flexible side-chain amino-benzene, design a series of 4 - to replace the aniline-based -6 - methoxy --7 -(2 - hydroxy replace C oxy) quinazoline compounds.

目的：通过各种化学合成方法完成目标化合物4--6-甲氧基-7-(2-羟基取代丙氧基)喹唑啉的合成并对目标化合物进行结构修饰，以期获得高活性的表皮生长因子受体酪氨酸激酶抑制剂。

The characteristics of quinazoline epidermal growth factor receptor inhibitors were briefly described in this paper, and the mechanism of receptor-tyrosine kinase inhibitor was also introduced. The synthesis of this kind of new compound was studied, and the synthetic route was redesigned and the method was modified.

本论文简述了受体酪氨酸激酶小分子抑制剂的发展概况，详细介绍了新型喹唑啉类表皮生长因子受体抑制剂，着重研究了该类化合物的合成，设计并打通了合成路线，同时又合成了25个新化合物。

RESULTS: A germacrane sesquiterpenoid, incaspitolide D (1), along with-N-benzoylphenylalanine--2-benzamido-3-phenyl- propyl ester (2), indole-3-carboxylic acid (3), apigenin (4), diosmetin (5) and luteolin (6) was isolated. CONCLUSION: Compounds 1-5 were isolated for the first time from Vernonia patula.

结果：分离到1个牻牛烷型倍半萜内酯， 1个苯丙氨酸衍生物、1个生物碱和3个黄酮化合物，根据波谱数据和X-衍射分析分别鉴定为：incaspitolide D (1)，-N-苯甲酰基苯基丙氨酸–-2-苯甲酰氨基–3-苯基丙酯(S-N-benzoylalanine-–2-benzamido-3-phenylpropyl ester， 2；吲哚-3-羧酸(indole-3-carboxylic acid， 3)；香叶木素(diosmetin， 4)，芹菜素(apigenin， 5)和木犀草素(luteolin， 6)。

Thirty-one new chiral phosphorus compounds have been synthesized starting from D-camphor,-alpha-phenylethylamine,-Betti base,-1-(4-nitrophenyl)-2-amino- propane-1,3-diol, L-amino acids (such as serine, phenylalanine, proline etc.) and their application as organocatalysts in asymmetric trimethylsilylcyanation of aldehydes and asymmetric borane reduction of prochiral ketones and ketimines were investigated.

该项目从D-樟脑、-alpha-苯乙胺、-Betti碱、-氯酶胺、L-氨基酸（如丝氨酸、苯丙氨酸、脯氨酸等）出发合成了31个新的手性磷化合物，研究了它们作为有机催化剂在醛的不对称硅氰化反应、潜手性酮的不对称硼烷还原反应以及亚胺的不对称硼烷还原反应中的催化效果。

Thiols are also active in the catalytic sites of enzymes,and play important roles in metabolic pathways.

细胞内巯基化合物(包括半胱氨酸、高半胱氨酸和还原型谷胱甘肽等)在维持生命体系的氧化还原动态平衡方面起着重要的作用，它们是与酶活性有关的最具有反应性的官能团，并且在酶代谢过程中起着重要的作用。

Firstly, phenyliodine diacetate was immobilized to the 2% cross-linked polystyrene or the liner polystyrene resin. The more iodine the resin had, the lower conversion to phenyliodine diacetate. We made our endeavor to extend the range of useful application of polystyrene supported phenyliodine diacetate in organic synthesis:(1) the reagent was used as an effective reagent of carbonyl regeneration from oximes and semicarbazones of ketones.(2) the reagent was also applied to the synthesis of 1, 3, 4-oxadiazoles, 1, 3-disubstituted-2-pyrazoline, 2-arylbenzoxazole from aldehyde N-acylhydrazones, aldehyde hydoazones and phenolic Schiff's bases respectively.

首先，我们以2％交联的聚苯乙烯和线性的聚苯乙烯树脂为载体，制备了聚合物负载的二醋酸碘苯，通过研究发现：(1)聚苯乙烯二醋酸碘苯是酮肟、缩氨脲有效的去保护试剂，不仅芳香酮，脂肪酮和α，β不饱和酮的肟、缩氨脲也能顺利转化为相应的酮，实现酮基的再生；(2)我们还利用此试剂，分别与醛的N-酰基苯、N-酰基苯腙及邻羟基芳亚胺反应，在温和的条件下发生成环反应，以良好的产率生成1，3，4-噁二唑、吡唑啉和二取代苯并噁唑等杂环化合物；(3)聚苯乙烯二醋酸碘苯还可有效地将邻羟基芳酮的酰腙经氧化、重排成1，2-二酰基苯。

Methods: Five patients with parkinsonism or dystonia were assigned to general anesthesia using an modified endotracheal tube.

本实验依照人体实验之相关规定进行，五位患有帕金森氏症或肌张力异常的病人接受神经立体定位手术。

If you can benefit from this book, it is our honour.

如果您能从本书获益，这将是我们的荣幸。