酰胺化作用

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。

The amidation of C-terminal is crucial for its full biological activity.

其C末端的酰胺化对它完整的生物活性起重要作用。

The glutamine synthetase produced by the engineering bacteria can specially act on NH4 and aminoglutaric acid, the durability to the high concentration ammonium ion has been distinctively improved because of the dissolution of adenosine acylation modification, the major bottleneck of glutamine with enzymatical production has been solved, and the concentration of the obtained glutamine can reach 47.6g/L.

本发明工程菌产的谷氨酰胺合成酶可专一性的作用于NH 4 和谷氨酸，且因解除了腺苷酰化修饰作用对高浓度铵离子的耐受能力显著提高，解决了酶法生产谷氨酰胺的重要瓶颈，生成的谷氨酰胺的浓度最高达到47.6g/L。

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

Was synthesized from cyanoacetic acid and diethylamine via DCC coupling under mild conditions.

中间体5 的制备由氰基乙酸在二环己基碳二亚胺作用下经酰胺化一步制得，条件温和，收率较高，避免使用剧毒的氰化钠。

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。

A process for preparingp-fluo-2-(2-methyl-3-propionyl)-4-oxy-N,3-diphenyl-phenylbutylamide includes such steps as Friedle-Craft acylating of newly prepared phenylacetyl chloride and fluorobenzene under catalysis of AlCl3 to obtain 4-fluoro-phenylbenzyl ketone, brominating at carbonyl alpha position under catalysis of less AlCl3 to obtain alpha-bromo-4-fluo-phenylbenzyl ketone, and condensing with isobutyryl acetanilide under action of sodium ethoxide.

本发明涉及一种制备对氟－2－(2－甲基－3－氧丙基)－4－氧－N，3－二苯基－苯丁酰胺(1)的方法，其包括以下步骤：新制的苯乙酰氯与氟苯在AlCl3催化下进行Friedle－Craft酰化反应，得到对4－氟－苯基苄基酮(4)；化合物(4)在少量AlCl3催化下进行羰基α位溴化，得到α－溴－4－氟－苯基苄基酮(5)；然后(3)异丁酰乙酰苯胺在乙醇钠作用下与化合物(5)进行缩合。

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。

In acid pulp, the depressing abilities of reagents on diaspore are in the order of hydroxamic acid starch＞dialdehyde starch＞carboxymethyl starch＞cationic starch＞primary starch. In addition, hydroxamic acid starch and carboxymethyl starch can activate kaolinite without influence on the recoveries of pyrophyllite and illite, so the two reagents have great potential and prospect to be the depressant of diaspore and the activator of kaolinite in bauxite reverse flotation.(3) By oximation of the copolymer of acrylamide and methyl acrylate, hydroxamic acid polyacrylamide is synthesized.

3对丙烯酰胺和丙烯酸甲酯的共聚物肟化制得氧肟酸聚丙烯酰胺，将它同非离子聚丙烯酰胺、阴离子聚丙烯酰胺、阳离子聚丙烯酰胺和两性聚丙烯酰胺分别应用于四种矿物的单矿物浮选试验，结果显示，改性聚丙烯酰胺对一水硬铝石、高岭石和伊利石均具有活化作用，其中，药剂对高岭石的活化最强，使它的回收率在整个pH值范围达到80％左右，在一定pH条件下超过一水硬铝石的回收率，解决了高岭石难浮选的问题。

Results showed that there were the morphological changes of mitochondria, such as vacuolization, degeneration and cristae swelling or disappearance, in HT-29 cells treated by C2-ceramide for 24 hours. Under the fluorescence microscope, mitochondria of apoptotic cells aggregated and emitted red fluorescence, however, mitochondria of normal cells emitted green fluorescence. The mitochondrial membrane potential began to decrease after 6 hours in HT-29 cells treated with C2-ceramide in time and dose dependent manner.

结果显示C2-神经酰胺作用HT-29细胞24小时，线粒体发生空泡化、变性、嵴肿胀或消失等形态学改变；此时荧光显微镜下可观察到线粒体聚集，发出红色荧光，而正常细胞线粒体发出绿色荧光。C2-神经酰胺作用细胞6小时，线粒体膜电位即开始降低，呈时间-剂量-效应关系。

The split between the two groups can hardly be papered over.

这两个团体间的分歧难以掩饰。

This approach not only encourages a greater number of responses, but minimizes the likelihood of stale groupthink.

这种做法不仅鼓励了更多的反应，而且减少跟风的可能性。