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During the manufacturing of the critical intermediate cephalosporin nucleus --7-amino-3-chloro-cephalosporanic acid diphenylmethyl ester hydrochloride salt, first the feasibility of the one-pot synthetic route of open loop, closed loop and ozonization when chlorine is passed over is qualified by experiments. Then the critical factors that will influence this reaction are studied as follows: the mol ratio of triphenyl phosphite and Diphenylmethyl 3-hydroxy-7-phenylacetaminoceph-3-em-4-carboxylate-l-oxide is four to one; the quantity of the stablizer should be at least more than two to one. The temperature of the system must be 25℃ when chlorine is passed over so that the hydrochloride can be precipitated to obtain cephalosporin nucleus of cefaclor--7-amino-3-chloro-cephalosporanic acid diphenylmethyl ester hydrochloride salt.

在制备关键中间体头孢母核7-氨基-3-氯头孢烷酸二苯甲酯盐酸盐时,先通过实验验证把开环、闭环、臭氧化三步在通入氯气时并为一锅煮的合成路线的可行性之外,又研究了影响该反应的几个重要因素:亚磷酸三苯酯与3-羟基-7-头孢烷-5-亚砜-2-甲酸二苯甲酯的摩尔比为4:1;稳定剂2-甲基-2-丁烯的用量至少大于2:1,通入氯化氢气体时体系温度在25℃时盐酸盐则能够顺利析出,获得头孢克洛的头孢母核—7-氨基-3-氯头孢烷酸二苯甲酯盐酸盐。

In the fifth chapter, six compounds formed between nitrogen-containing ligands such as 2, 2'-bipyridyl, isonicotinamide and 1, 4, 8, 11-tetraazacyclotetradecane and the solution cadmium sulfonates such as 1, 5-naphthalenedisulfonate, 2, 6-naphthalenedisulfonate, 4, 4'-bipenyldisulfonate and 4, 4'-penyletherdisulfonate have been synthesized and structurally characterized. Besides, another compound has been synthesized with cadmium carbonate reacting with 1, 5-naphthalenedisulfonate acid.

第五章以2,2'-联吡啶、异烟酰胺和1,4,8,11-四氮杂环十四癸烷与含有Cd〓和1,5-萘二磺酸根离子、2,6-萘二磺酸根离子、4,4'-联苯二磺酸根离子和4,4'-苯醚二磺酸根离子的水溶液反应,合成了六个化合物,另外以1,5-萘二磺酸与碳酸镉反应合成出一个化合物。

By means of GPC,IR,GC-MS,~(13)CNMR,~1HNMR,Methylation analysisetc,structural properties of PST-1 were identified as follows:The Mwof PST-1 was 3.44×10~6 Da and its optical rotation was _D~(20)=+0.110°(c0.1, H_2O); PST-1 constituted 8 simple sugars and the molar ratio was 2,4-Dimethoxy-Mannose:Rhamnose:Ara-binose:Xylose:Galactose:D-Galacturonic acid:Mannose:D-glucuronic acid=2%:5%:24%:9%:3%:1%:46%:10%;The chief bone of PST-1 was 1,3,6-linked-β-D-Man residue and the side chains contained Furanoid and Pyranoid residues.

结合GPC、旋光度测定、IR、GC-MS、~(13)CNMR、~1HNMR、高碘酸氧化法、Smith降解以及甲基化方法等分析测试方法,得到PST-1的单糖组成及结构表征,实验结果如下:红豆杉多糖PST-1是重均分子量为3.44×10~6 Da的支链多糖,旋光度为20D=+0.110~0(c0.1,H_2O);PST-1单糖组成为:2,4-Dimethoxy-Mannose:Rhamnose:Arabinose:Xylose:Galactose:D-Galacturonic acid:Mannose:D-glucuronic acid=2%:5%:24%:9%:3%:1%:46%:10%;PST-1的骨架结构为:具有1,3,6-连接的β-D-甘露糖残基骨架,侧链分枝包括非还原末端的呋喃型α-L-阿拉伯糖残基、吡喃型α-L-阿拉伯糖残基、β-D-木糖残基、β-D-甘露糖残基、2,4-二氧甲基-β-D-甘露糖残基和α-D-葡萄糖醛酸残基;侧链的糖残基也可能存在2,5-二氧-取代呋喃型α-L-阿拉伯糖基、3-氧-取代的β-D-木糖残基、6-氧-取代的α-D-半乳糖醛酸残基、6-氧-取代的α-D-半乳糖残基、4-氧-取代的α-D-葡萄糖醛酸残基和2-氧-取代的α-L-鼠李糖残基,同时后者也可能穿插在主链上。

Our data are showed that apoptosis parameters including DNA fragmentation, nuclear morphological change and sub-G1 fraction, appeared after 24 h by 5 μM rottlerin treatment. Furthermore, rottlerin caused a decrease in 72% of ODC protein expression and an increase in threonine, rather than serine and tyrosine dephosphorylation on ODC enzyme compared with the control after incubation for 10 h. To determine whether ODC could down-regulate rottlerin-induced apoptosis, HL60 cells were stably transfected with ODC cDNA. HL60-ODC cells exhibited a 2.5-fold increase in ODC protein compared with vector only (HL60-pcDNA3) or HL60 cells.

在我们筛选天然化合物实验中,发现rottlerin抑制鸟胺酸去羧化活性最具成效,之前的研究人员已知蛋白激Cd调节鸟胺酸去羧化的活性,因此在人类白血病HL60细胞处理rottlerin的实验中发现加入rottlerin二十四小时后,细胞进行计划性死亡,并可侦测到DNA片段、细胞核浓缩及sub-G1提增;而细胞处理药物十小时后与控制组细胞比较,观察到鸟胺酸去羧化的蛋白表现与活性下降50﹪以上;除此以外,测定鸟胺酸去羧化去磷酸化的情况,发现於酥胺酸位置有显著差异,而丝胺酸和酪胺酸位置并无差异。

The important role of hydroxycinnamic acids,i.e.,caffeic acid, chlorogenic acid,sinapic acid,ferulic acid,3-hydroxycinnamic acid (3-HCA) and 4-hydroxycinnamic acid(4-HCA) as the pBR322 plasmid DNA-Cleaving agents in the presence of Cu ions was investigated.

我们研究了羟基肉桂酸衍生物即咖啡酸、绿原酸、芥子酸、阿魏酸、3-羟基肉桂酸(3-HCA)和4-羟基肉桂酸(4-HCA)在Cu存在下诱导pBR322质粒DNA链断裂损伤情况,结果发现HCAs的促氧化活性与它们的分子结构有密切的关系,具有邻二羟基结构和邻二甲氧基羟基结构的化合物表现出了更高的促氧化活性,其中CaA的活性最高。

Aggregation Behavior and the Hard Water Resistant Ability of Linear Alkylbenzene Sulphonate :MesoDyn Simulation and Quantum Calculation Study The quantum calculation and MesoDyn simulation were combined in this paper, the Critical Micella Concentration difference of LAS and AS was studied by the simulation, and aggregation morphology as well as aggregation behavior of linear alkylbenze sulfonate in aqueous solution was investigated by MesoDyn simulation in the presence and absence of shear.

水溶液中直链烷基苯磺酸盐的介观模拟及其抗硬水能力的量子化学计算将介观模拟和量子化学计算方法相结合,通过模拟的方法从介观角度研究了十二烷基苯磺酸盐和十二烷基磺酸盐临界聚集浓度的差异,考察了LAS水溶液体系的聚集形貌以及微相分离时发生的复杂行为。

Their structures were characterized as usnic acid,evinic acid,perlatolic acid,olivetoric acid,2-hydroxyl-4-methoxyl-6-pentyl benzoic acid and 2,4-dihydroxyl benzoic acid,respectively.

结果从太白花的石油醚部分得到6个化合物,分别鉴定为:松萝酸、去甲环萝酸、珠光酸、漂红梅衣酸、2-羟基-4-甲氧基-6-正戊基苯甲酸和2,4-二羟基-6-正戊基苯甲酸。

AIM To investigate whether the human pro- lidase possesses the G-type organophosphate hydrolyzing enzyme activity besides its ability to catalyze the hydrolysis of the dipeptides bearing a proline residue at the C-terminus.

目的研究人氨酰基脯氨酸二肽酶除催化水解C端为脯氨酸残基的二肽外,是否还有G类有机磷化合物水解酶活性。

A new type of polyaspartic esters secondary amine called PAE-b was prepared from prime amine 4,4'-methylenebis and dialkyl maleates via a Michael Addition Reaction.

通过伯胺4,4'-二氨基环己基甲烷与马来酸二乙酯的Michael加成反应,合成1种新型聚天门冬氨酸酯仲胺。

Optimal experimental conditions were as follows: 2μL toluene microdrop exposed for 20min in a 3mL aqueous sample placed in 4mL vial and stirred at 600rpm/min.

研究了单滴液相微萃取与气相色谱测定水中以酞酸二甲酯和酞酸二丁酯为代表的酞酸酯类化合物。

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