胺化产物

Background and Objective The goals of this study were to label the antisense oligodeoxynucleotidesindirectly by Chloramine Tmethod and Iodogen method,then to discuss the labeling yields、radiochemical purity、specific activity and stability in different conditions.

目的与研究背景：本课题采用氯胺-T法和Iodogen法两种标记方法进行反义寡脱氧核苷酸的125I间接标记对比研究，并在两种方法中分别探讨不同反应条件下的标记率及标记产物的放化纯、比活度和稳定性。

Background and Objective The goals of this study were to label the antisense oligodeoxynucleotides indirectly by Chloramine T method and Iodogen method, then to discuss the labeling yields、radiochemical purity、specific activity and stability in different conditions. We discussed the right labeling method and conditions in order to lay the experiment foundation of the antisense medicament labeled by iodine for clinical application.

目的与研究背景：本课题采用氯胺-T法和Iodogen法两种标记方法进行反义寡脱氧核苷酸的125I间接标记对比研究，并在两种方法中分别探讨不同反应条件下的标记率及标记产物的放化纯、比活度和稳定性。

Hepatic sinusoid capillarization plays an important role in occurrence of portal hypertension. The fenestra of endothelial cells in hepatic sinusoid reduces and the diameter of fenestra decreases. The formation of basement membrane impaires the substance exchange between blood and hepatic cells,which results in oxygen deficiency, metabolic product accumulation and cell necrosis.

肝窦毛细血管化在硫代乙酰胺诱导的肝硬化门脉高压发生中起重要作用，肝窦内皮细胞窗孔减少并减小，内皮细胞下基底膜形成使肝细胞与外界物质交换减少，导致细胞缺氧、代谢产物聚集，肝细胞坏死，最终导致门脉高压的发生。

In chapter 4 an abnormal reaction that the nitro group of 1-aryl-2-nitroethenescan be easily replaced by the organic moity of FG-RZnI using Ni〓 and tertiaryamine as catalyst was first given. The experimental results show that in the presenceof catalytic amount of Ni〓 and tertiary amines, the reaction of FG-RZnI andl-aryl-2-nitroethenes give the substitution products l-aryl-l-alkene, instead ofMichael addition products.

通过实验发现，在催化量的Ni〓及叔胺催化下， l-硝基-2-芳基乙烯与烷基碘化锌并不进行Michael加成反应，而是发生1-硝基-2-芳基乙烯中硝基被取代的反应，生成了高产率的1-芳基-l-烯烃，由于此反应的原料易得、反应条件温和、产物的产率高，因而是合成l-芳基-1-烯烃的有效方法。

Benzyloxy benzoyldimethylsulfoxide was prepared by the reaction of ethyl 4-benzyloxybenzoate and dimethyl sulfoxide in the presence of sodium hydride, followed by Pummerer reaction with concentrated hydrochloric acid to afford eo-hydroxy-co-thio-methyl-(4/-benzyloxy) acetophenone, which reacted with urea, thiosemicarbazide, semicarbazide hydrochloride and o-phenylenediamine to give imidazolidine-2,4-dione, l,2,4-triazine-3- one and quinoxaline derivatives, respectively.

本文用4-苄氧基苯甲酸乙酯和二甲亚砜为原料，在氢化钠存在下反应，合成了(4′-苄氧基)-苯甲酰基-二甲亚砜。研究了该亚砜在浓盐酸的存在下发生的Pummerer重排反应，用重排产物ω-羟基-ω-甲硫基-(4′-苄氧基)-苯乙酮分别与尿素、氨基脲、氨基硫脲和邻苯二胺反应合成了2，4-咪唑啉-二酮、1，2，4-三嗪-3-酮、喹喔啉等含氮杂环化合物。

The auxiliary can be recovered in high yield (81%) only by filtering and recrystallization. Besides, some other aldehydes have been chosen to test the enantioselectivity of N,N\'-dibenzyl tartamide, in comparison with two other allylaborates reagents developed previously by Roush and Brown, respectively. The results show that %e.e. of homoallylic alcohol is superior to that of the former, and approaches the Brown reagent.

产物经S_N2反应得瑞格列萘中间体-甲基烯丙基-2-氯苯基-叠氮甲烷(17)；同时，将筛选出的新型手性配体N-苄基酒石酸二酰胺用于其他几种醛(正丁醛，异戊醛和环己醛)的不对称烯丙基化反应，并与广泛应用的Roush配体(22)和Brown配体(27)相比较，发现其立体选择性优于Roush配体，并接近Brown配体，但明显具有可回收利用的优势。

For it is rubor after damaging to the closing soft tissue, getting swollen, getting hot aching and model of functiolaesa these bed solicit and there is no fracture,no skin damaged, we designed the corresponding experiment, namely the law of hot board causes little mouse\'s painful experiment of threshold of pain; Freun\'s complete adjuvant caused the swollen experiment of big mouse\'s foot;The xylene caused the swollen experiment of little mouse\'s ear; Invigorating blood circulation silt experiment that changes the sex that the rheology appearance examines the blood and flows with the blood; Useing the high performance liquid chromatography-electrochemistry Detected monoamine neurotransmitters transmitter in the brain and serum; the experiment of immunohistochemistry measured the proto-oncogene C-FOS expresses.

针对闭合性软组织损伤后的红、肿、热、痛及功能障碍的典型临床体征，加上无骨折、无皮肤破损的特点，我们设计了相应的实验，即热板法致小鼠疼痛的痛阈实验；福氏完全佐剂(Freun\'s complete adjuvant，FCA)致大鼠足肿实验；二甲苯致小鼠耳肿实验；用血流变仪测血液流变性的活血化瘀实验；运用高效液相色谱—电化学(high performance liquid chromatography-electrochemistry Detection HPLC-ECD)法测量大脑及血清中单胺类神经递质的实验以及免疫组织化学法检测原癌基因C-FOS蛋白产物表达的实验。

Results show that, by using thionyl chloride and N,N-dimethyl formamide as chlorinating reagent and dichloromethane as solvent and taking -15℃ as reaction temperature, Z-iomer crystals with pale white color and stable to temperature can be obtained with an overall yield of 70%.

以2-（2-氨基噻唑－4-基）－2-甲氧亚氨基乙酸为原料，经盐酸化、氯代等反应合成了Z-2-（2-氨基噻唑－4-基）－2-甲氧亚氨基乙酰氯盐酸盐；氯代时以用亚硫酰氯和N，N-二甲基甲酰胺的混合物代替五氯化磷作氯化剂，并考察了温度和溶剂对氯代产物中Z-异构体和E-异构体收率的影响。

Methods: Streptomycin and the derivatization reagent o-phthalaldehyde occur Amine Acetalization generating derivative product with UV absorption and determined the absorbance in special wave length, obtained streptomycin residues in samples then compare with high-performance liquid chromatography.

将试样与衍生化试剂邻苯二甲醛进行胺缩醛反应，即化学衍生处理，生成具有特定波长的紫外吸收的衍生产物，测定其吸光度，求出样品中链霉素残留量，并与高效液相色谱法比较。

First, the geometry optimization for 1-phenyldibenzophosphole and triphenylphosphine were carried out using quantum chemical AM1 method.

用量子化学AM1方法优化了1-苯基二苯并膦和三苯基膦的几何构型，比较了两种化合物的电子结构和空间结构，发现PDBP作为羰基合成铑膦催化剂的配体要优于三苯基膦；系统研究了PDBP的合成方法，其最佳合成条件为：在无水无氧的条件下，采用二乙胺锂与溴化四苯基膦摩尔比为3，反应温度为22 ℃，反应5 h，反应后酸化， pH值为1～2，产物收率可达到85％～88％。

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。