酰化作用

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。

RBL-2H3 cells expressing formyl peptide receptor being stimulated with two polypeptides was used as model system to characterize the chips' performance. As a result, fMLF triggered chemotaxis, receptor internalization and calcium mobilization, while GSH had no effect on the cells.

以含有不同氨基酸序列的多肽作用表达甲酰肽受体的RBL-2H3细胞为模型体系，对芯片组性能予以验证，结果表明，N-甲酰肽物质能够刺激细胞发生趋化运动、受体内吞和钙离子释放，而作为阴性对照的还原型谷胱甘肽无此能力。

E. value of productions were detected by high performance liquid chromatography. Results The chiral aminoalcohol ligand compound Ⅰ can promote the asymmetric allylation of acylhydrazones and the yield was 57%; The highest values of e. e. obtained for this reaction was 22%.

结果 手性氨基醇配体化合物Ⅰ能够促进烯丙基三氯硅烷和酰腙的烯丙基化加成反应，在它的辅助作用下，烯丙基化加成产物的产率可达到57%，对映体过量值最高达到22%。

A series of 2-acetylformanilides were prepared,followed by thiolation with Lowesson reagent to afford 2-acetylthioformanilides,which further reacted with Mn3·2H2O in glacial acetic acid under microwave irradiation to afford 2-acetyl benzothiazole s.

合成了一系列的硫代酰胺，研究了它们在微波辐射醋酸锰作用下发生氧化自由基环化反应，成功地合成了一系列2-乙酰基苯并噻唑衍生物，其结构经红外光谱、核磁共振谱和质谱得到了证实

This dissertation is mainly focused on the reactivity of methylenecyclopropanes and comprises six parts. 1 The reactions of methylenecyclopropanes with phenylsulfenyl chloride, phenylselenyl chloride and diphenyl diselenide; 2 The coupling reactions of the ring-opening products derivated from methylenecyclopropanes; 3 The palladium-catalyzed ring-enlargement of mono-aryl group substituted methylenecyclopropanes to cyclobutenes. 4 The gold-catalyzed domino ring-opening and ring-closing hydroamination of methylenecyclopropanes with sulfonamides; 5 The Lewis acid-catalyzed reactions of mono-aryl group substituted methylenecyclopropanes with diethyl ketomalonate in the presence of water; 6 The iodobenzene diacetate mediated novel 1,3-dipolar cycloaddition of methylenecyclopropanes, vinylidenecyclopropanes, and methylenecyclobutane with phthalhydrazine.

本论文主要研究了亚甲基环丙烷类化合物的一些化学反应性能，共由以下六部分组成：1、亚甲基环丙烷类化合物与苯硫氯、苯硒氯及二苯基二硒的反应；2、亚甲基环丙烷类化合物开环产物的偶联反应；3、单芳基取代的亚甲基环丙烷类化合物在钯催化剂作用下的扩环反应；4、金化合物催化磺酰胺对亚甲基环丙烷类化合物的串联开环关环氨氢化反应；5、路易斯酸催化亚甲基环丙烷类化合物与丙酮二羧酸二乙酯在有水存在下的反应；6、醋酸碘苯促进的亚甲基环丙烷类化合物、亚乙烯基环丙烷类化合物及亚甲基环丁烷类化合物与邻苯二甲酰肼的新型1，3-偶极环加成反应。

The stable or unstable state of the montmorillonite-water dispersion is mainly effected by the properties of montmorillonite, water, and stabilizers as well as their interactions, while the type, the structure, the properties and the concentration of the stabilizer play dominate roles. Based on the molecular designing clues, this research selected three sulfonated copolymers as the stabilizers, i.e. the sodium 2-acrylamido-2-methyl-1propane sulfonate /acrylamide /disodium itaconate terpolymer, the AMPS/AM/N-vinyl pyrrolidone terpolymer and the sodium styrenesulfonate /IA copolymer. The preparation and characterization of the sulfonated copolymers were discussed, the high-temperature stability of the montmorillonitewater dispersion was characterized with the rheology, the filtration, the particle size distribution, the electrostatic properties, and the adorption of the sulfonated copolymers onto montmorillonite particles. At the same time, a systematic mechanism of the hightemperature stabilization of the dispersion was presented.

本文构筑了分子设计的思路，选取AMPS(2-丙烯酰胺基-2-甲基丙磺酸钠)/AM/IA三元共聚物、AMPS/AM/NVP三元共聚物和SSA/IA二元共聚物等三种磺化共聚物作为蒙脱土-水分散体系的高温稳定剂，进行了磺化共聚物稳定剂的制备与表征；从流变学、滤失性能、粒度分布、电性质以及磺化共聚物在蒙脱土上的吸附作用等方面，对蒙脱土-水分散体系的高温稳定性进行了研究，考察了蒙脱土-水分散体系的高温稳定性能，同时提出了高温稳定机理。

Macrocycle with one pyridyl unit and one aryl oxdiazole unitCondensation of Ts-amino acids with 2,6-bishydroxymethyl pyridinegave di-esters in the presence of DCC and TsOH in pyridine. DMAP,another acylation catalyst was also discussed in our esterification.

二。含一个吡啶环和一个二苯基噁二唑单元：直接采用Ts保护的氨基酸与吡啶二醇在吡啶-TsOH反应体系中，在DCC作用下生成吡啶二醇二酯，讨论了酯化过程中不同酰基化试剂的应用。

Research result indicated that the cooperative effect between swell and precursor is main factor for the nanoparticle loaded in Nafion, and moreover, polarity of solvent and water content in Nafion also affects the load largely. To improve away the surface concentration of CdS nanocrystal on two side of membrane for general preparation, thioacetamide was first used as a precursor instead of inorganic sulfur source(H2S and Na2S) in synthesis of CdS nanocrystal. The assembly mechanism for several sulfur source had been studied, and CdS/Nafion with the character of homogeneous disperse had been prepared, which is fit for mass transmission in photocatalitic reaction. Following the investigation of several crystallizing way, simple and reliable hydrothermal-crystallizing was found. According to this way, maximal TiO2 load in Nafion achieved 43%. Activity of TiO2/Nafion or CdS/Nafion as a photocatalyst was explored initially for disintegrating liquid contamination. Maximal decompose rate achieved 86% under condition of this research.

研究结果表明：Nafion膜对纳米粒子负载量的主要影响因素是溶胀作用与前驱体协同效应，同时溶剂极性和薄膜含水量对负载量也影响相当大；本课题首次使用硫代乙酰胺代替传统无机硫源（H2S、Na2S）合成CdS纳晶，研究了各种硫源的组装机理，克服了常规技术存在的CdS纳晶趋于膜表面富集的缺点，得到了有利于光催化传质需要的体相均匀分布CdS/Nafion；研究了多种Nafion膜内纳米粒子晶化途径，找到了简单可靠的水热晶化法，TiO2纳晶最高负载量达43％；初步探索了TiO2/Nafion、CdS/Nafion作为光催化剂降解水中模拟污染物的活性，在本实验条件下最高降解率达86％。

The result of potassium malonyloxyborohydride as a new hydroboration reagent reacts with terminal alkenes and alkynes is described.

介绍新的硼氢化试剂丙二酰氧基硼氢化钾与链端烯炔烃的作用，烯烃的硼氢化物在PTC条件下，插入∶CCl2 ，可得饱和羧酸；炔烃则难以与之硼氢化。

N-methylmaleimide was prepared by using dimethyl sulfate as methylation reagent.The paper investigated the addition of N-methyl-3,4-dibromomaleimide and indolylmagnesium bromide,and then 2-bromo-3-(1H-indolyl-3-yl)-N-methylmaleimide and 3,4-bis(1H-indolyl-3-yl-)-N-methyl-maleimide were obtained.

对吲哚在溴乙烷和镁作用下生成吲哚溴化镁，而后与3，4－二溴－N－甲基马来酰亚胺的加成反应进行了研究，合成了2－溴－3－(1H－吲哚－3)－N－甲基马来酰亚胺，并对反应条件进行了改进，研究了反应温度和原料配比对反应的影响。

We have no common name for a mime of Sophron or Xenarchus and a Socratic Conversation; and we should still be without one even if the imitation in the two instances were in trimeters or elegiacs or some other kind of verse--though it is the way with people to tack on 'poet' to the name of a metre, and talk of elegiac-poets and epic-poets, thinking that they call them poets not by reason of the imitative nature of their work, but indiscriminately by reason of the metre they write in.

索夫农 、森那库斯和苏格拉底式的对话采用的模仿没有一个公共的名称；三音步诗、挽歌体或其他类型的诗的模仿也没有——人们把&诗人&这一名词和格律名称结合到一起，称之为挽歌体诗人或者史诗诗人，他们被称为诗人，似乎只是因为遵守格律写作，而非他们作品的模仿本质。

The relationship between communicative competence and grammar teaching should be that of the ends and the means.

交际能力和语法的关系应该是目标与途径的关系。