缩氨酸

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。

hydantoin was synthesized from diethyl malonate comprising condensation with 1, 2-dichloroethane, ammonolysis to diamide, Hoffmann degradation to give 5-cyclopropanespirohydantoin, and ring-opening with 40% hydrobromic acid.

以丙二酸二乙酯为原料，先与1， 2-二氯乙烷缩合生成1， 1-环丙烷二羧酸二乙酯，再经氨解生成1， 1-环丙烷二甲酰胺，然后在次氯酸钙溶液中进行Hoffmann降解成环生成5-环丙螺海因，最后在40%氢溴酸中开环得到5-溴乙基海因。

EDD and NEDD of external iliac artery in vivo (measured with high-resolution ultrasound), serum lipids, NO, NOS, plasma ET, ADMA, symmetric dimethylarginine and L-arginine, the area of AS plaque in thoracic aorta (dyeing with Sudan Ⅳ), the degree of AS lesion in abdominal aorta and external iliac arteries, NOS activity on the wall of the abdominal aorta, the expression of iNOS mRNA and eNOS mRNA on the wall of the abdominal aorta and the contractive and dilatant functions of abdominal aorta and external iliac arteries in vitro; B. the activities of dimethylarginine dimethylaminohydrolase in kidney (including the establishment of the determining method). 3. In the third part of the study, normal aorta strips were used. The following were surveyed: their response to using ADMA alone, influence of treating with ADMA, intervention of polydatin, influence of using ADMA and PD together on Emax and Kd that were contracted by PE.

第5组为未给药组。2、观察指标：A、各组髂外动脉EDD和NEDD、血脂、血清NO和NOS活性、血浆ET、ADMA、SDMA和L-精氨酸水平、胸主动脉AS斑块面积、腹主动脉和髂外动脉AS病变积分、腹主动脉壁NOS组织化学染色和eNOS mRNA和iNOS mRNA表达及离体腹主动脉与髂外动脉舒缩功能。B、各组兔肾DDAH活性。3、离体做正常主动脉条对单用ADMA的反应、PD和ADMA对PE收缩效应的影响及PD预处理对受ADMA作用的正常主动脉条PE收缩反应的影响(包括对Emax和Kd值的影响)。

The synthesis of the pentacyclic skeleton of Et-743 and the construction of the five chiral centers thereof.1. The core pentacyclic skeleton of phthalascidin was constructed with L-dopa as the starting material via thirteen steps. First, two basic synthons, the C-1 functionalized tetrahydroisoquinoline compounds 8 and N-protected Z-dopa derivative 9, were prepared from L-dopa. They were coupled via amide bond to form the dipeptide compounds 10, which were the first key intermediates. Then the primary hydroxyl groups were transformed into the corresponding amino aldehydes 11 via Swern oxidation. Followed by the intramolecular Pictet-Spengler cyclization, the pentacyclic compounds 12 were synthesized.

五环骨架的构建及五个正确手性中心的确立：1.1我们以L-多巴为起始原料，经过多步官能团保护和转化合成了基本结构单元8然后和苯丙氨酸衍生物9，通过缩合反应生成酰胺中间体10，经Swern氧化得到醛化合物11，然后再次利用分子内改良的Pictet-Spengler反应一步构建c，d两环，得到五环骨架化合物12，最后，实现了21-位羰基向氰基的转化，得到了C-1位官能化的化合物14，化合物14不但具有和Et-743一致的五环骨架，而且分子中五个手性中心立体构型也与其完全相同：其中，3，位和13，位的手性中心由原料L-多巴带入，而1，位，11，位和21，位手性中心则通过不对称诱导而确立。

reitman method to measure ALT and AST; bilirubin oxidase method to measure total bilirubin and conjugated bilirubin; biuret method to measure serum general protein; bromocresol purple method to measure serum albumin; enzymic colorimetric method to measure serum bile acids; benzyl aldehide azo naphthol method to measure monoamine oxide.

赖氏法。测定 ALT 和 AST；胆红素氧化酶法测定总胆红素和结合胆红素；双缩脲法测血清总蛋白；溴甲酚紫法测定血清清蛋白；酶比色法测定血清胆汁酸；苄醛偶氮萘酚法测定单氨氧化酶

The formation of charge transfer complex was studied in the first part. The second part includes the synthesis and characterization of the acrylated unsaturated polyester and the kinetic studies on the Ar-UPE/ triethylene divinyl ether (DVE-3) photocuring system, the rheology and properties of film after photocuring. The third part includes the synthesis and characterization of the urethane modified unsaturated polyester and the kinetic studies on the PU-UPE/DVE-3 photocuring system, the rheology and properties of film after photocuring. The fourth part includes the synthesis and characterization of the vinyl ether end capped polyurethane and the kinetic studies on the VE-PU/DVE3 photocuring system, the rheology and properties of film after photocuring.

整个研究工作分为四个部分：一是电荷转移复合物的研究；二是丙烯酰氧基化不饱和聚酯的合成，表征，Ar-UPE/二缩乙二醇二乙烯基醚（DVE-3）体系光固化动力学研究以及Ar-UPE/DVE-3体系流变性能和光固化后涂膜综合性能的研究；三是氨酯改性的不饱和聚酯的合成，表征，PU-UPE/DVE-3体系光固化动力学研究以及该体系光固化后涂膜综合性能的研究；四是乙烯基醚封端的聚氨酯的合成，表征，VE-PU/马来酸二甲酯体系光固化动力学研究以及VE-PU/DMA体系流变性能和光固化后涂膜综合性能的研究。

Ab initio and density functional theory (B3LYP) in G98 were employed to study the following four direct aldol reactions between acetone and isobutyraldehyde or 3,3-dimethylbutyric aldehyde or benzaldehyde or 4-bromo-phenyl aldehyde catalyzed by-proline .

中文摘要：本文采用G98程序包中的从头计算方法和密度泛函方法计算研究了-脯氨酸催化丙酮与异丁醛、3，3-二甲基丁醛、苯甲醛及对溴苯甲醛的不对称直接羟醛缩合反应，共计四个反应体系。

Sodium oleoyl sarcosine was synthesized by the method of Schotten-Banmamm.

用肖顿－鲍曼(Schotten-Banmamm)缩合反应法合成油酰肌氨酸钠。

After administration of L-N〓-nitro-Arginine, a specific antagonist of NOS, it was found that the basal and stimulated NO release of blood vessels (aorta, internal carotid, renal and mensenteric artery) was decreased further. The increase of coronary blood flow stimulated by Ach was also reduced further, while the platelet aggregation degree and erythrocyte aggregation index increased significantly. Pathological examination indicated that aortic endothelium was destroyed, the blood vessels in cerebral, cardiac and renal tissues were hypertrophied further and some were almost occluded. The above fin dings resulted in SHR feeded with L-NNA having high incidence of stroke rate and high degree of renal cirrhosis when compared to control SHR. The infarct and hemorrhagic focuci in cerebral tissues, infarct focuci in cardiac tissues, atrophy and hyalinedegeneration of renal glomeruli and degeneration even necrosis of renal tubuli in renal tissues were al so found. The increase ratio of brain and heart to body weight and decrease ratio of kidney to body wei ght further demonstrated that the cerebral, cardiac and renal injuries were aggravated.

在上述结果的基础上进一步给予SHR NOS特异性拮抗剂左旋亚硝基精氨酸后，血管(胸主、颈内、肾及肠系膜动脉)NO基础释放及激动剂刺激释放进一步减少，Ach刺激冠脉流量的增加和胸主动脉内膜NOS活性也进一步减少，血小板聚集程度及红细胞聚集指数显著上升，病理切片显示胸主动脉内皮细胞破坏明显，脑心肾组织内的血管进一步增厚甚至几乎阻塞，导致饲L-NNA的SHR缺血性及出血性脑卒中发生率显著高于对照SHR，脑体重比显著升高；心肌内出现明显的缺血梗塞疤痕灶，心体重比显著升高；肾小球明显萎缩、玻璃样变性，肾小管也变性甚至坏死，使肾硬化程度显著增加呈颗粒性固缩肾，肾体重比也显著减少。

Breath, muscle contraction of the buttocks; arch body, as far as possible to hold his head, right leg straight towards the ceiling (peg-leg knee in order to avoid muscle tension).

呼气，收缩臀部肌肉；拱起身体，尽量抬起头来，右腿伸直朝向天花板（膝微屈，以避免肌肉紧张）。

The cost of moving grain food products was unchanged from May, but year over year are up 8%.

粮食产品的运输费用与5月份相比没有变化，但却比去年同期高8％。