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The originalprocedure has subsequently been replaced by milder and more environmentallyfriendly conditions. We tried to alkylate 3,4,5-trimethoxytoluene by2-allylphenylbenzyl ether in the presence of N-bromosuccinimide.

本实验是在溴代琥珀酰亚胺的作用下使2-烯丙基苯基苄基醚产生苄正离子,苄正离子亲电进攻3,4,5-三甲氧基甲苯从而进行傅氏烷基化反应的。

In part one, the reactions of some active fluorine-containing compounds such as 2, 2-dihydropolyfluoroalkanoic acids and ethyl 2-hydropolyfluoroalkenoates were studied and various fluorine-containing heterocyclic compounds were synthesized. Using 2, 2-dihydropolyfluoroalkanoic acids as the starting material, 4-fluoroalkyl quinolin-2-ols, 2- [ -1-hydropolyfluoro-1-alkenyl] -4H-3, 1-benzoxazin-4-ones, 1-aryl -4, 9-dihydro-3-fluoro-alkyl-1H-pyrazo [3, 4-b] quinolin-4-ones, 5-fluoroalkyl-12H-quin olino [2, 1-b] quinazolin-12-ones, 4-fluoroalkyl-1, 3-dihydro-1, 5-benzodiazepin-2-ones and 4-fluoroalkyl-2H-pyrido [1, 2-a] pyrimidin-2-ones were synthesized through its condensation reaction with anilines, anthranilic acid, N'-aryl-o-aminobenzamides, o-nitro aniline, o-amino pyridine and their derivatives and the subsequent transformations. 5-Fluoroalkyl isoxazolidines, 3-fluoro-3-fluoroalkylisoxazolidino [4, 3-c] quinolin-4-ones, 3-fluoroalkylisoxazolino [4, 3-c] quinolin-4-ones and 2-aryl-3per fluoroacylindoles were synthesized by inter-and intramolecular 1, 3-dipolar cycloaddition of fluorine-containing olefins and nitrones.

第二部分,我们研究了α,α-二氟苄基卤类化合物的亚磺化脱卤反应、产物的转化及全氟烷基亚磺酸盐与芳环化合物的全氟烷基化反应,发现全氟苄基碘或溴及α,α一二氟苄基溴在保险粉等亚磺化脱卤试剂引发下可生成相应的亚磺酸盐;全氟苄基亚磺酸盐与氯气或溴反应可生成全氟苄基磺酰氯或磺酰溴;在烯烃存在下,全氟苄基碘则与烯烃发生加成反应,生成相应的1:1加成产物;在三价醋酸锰的作用下,部分芳香化合物如茴香醚,二甲氧基苯,吡啶,喹啉等可以和过量的全氟烷基亚磺酸盐发生双全氟烷基化反应,反应表现出一定的区域选择性,产率良好。

Objective to evaluate the functional recovery of acute spinal cord injuried rats treated with exogenous wnt-3a signal protein administration and to explore its mechanism.methods moderate spinal cord contusion injury was made in 40 adult sprague dawley rats at t10.twenty rats served as contusion controls(group 1).twenty rats were treated with wnt-3a for three days after injury (group 2).the functional recovery of the rats was observed through basso,beattie,bresnahan open field locomotor score.rats were killed at 14 or 28 days after injury,then spinal cords were removed for histopathological examinations,and the expression of the bromodeoxyuridine plus neural cell markers was stained with immunohistochemical method.results rats of two groups receiving a contusive injury recovered substantial function within 1 week.by 28 days,rats in groups 2 scored 7.0 points better on the bbb scores than rats in group 1 group 2=16.94,after 28 days vs.

目的 研究外源性wnt-3a信号蛋白对脊髓损伤的修复作用,并探讨其作用机制。方法取40只成年雌性sd大鼠在t10节段制备适度脊髓挫伤模型。随机从中取20只为损伤对照组(group 1),另外20只为损伤治疗组(group 2)。脊髓损伤3天后用wnt-3a蛋白治疗。这些大鼠的功能恢复通过basso、beattie、bresnahan开放视野运动评分来观察。这些大鼠分批在损伤后14天或28天被处死,取出损伤节段脊髓用来组织病理学检查,同时用5-溴脱氧尿嘧啶核苷和神经细胞标记物进行免疫组化染色。结果两组大鼠在伤后一周运动功能有明显的恢复。不过,到损伤后28天,我们观察发现,损伤治疗组中的大鼠bbb评分比损伤对照组中的评分高出7.0分左右(group 2∶16.94±1.18,group 1∶9.89±1.29;p.05),光镜和电镜检查发现wnt-3a蛋白对髓鞘形成和轴突再生有一定的修复效果。

The reaction of 4-bromaophenol and geranic acid in the presecnce of p-TsOH afforded 4-bromophenolα-cyclogeranoate in which cyclization of geranic acid toα-cyclogeranic acid was followed by esterification ofα-cyclogeranic acid with p-bromophenol.

对溴苯酚与香叶酸在p-TsOH催化作用下发生了香叶酸向α-环香叶酸环化、α-环香叶酸环与对溴苯酚的酯化,得到了唯一产物α-环香叶酸对溴苯酯,产率68%。

The first synthetic route uses 1,2,4-trimethoxybenzene and chloroacetonitrile in forming 2,4,5-trimethoxy-a-chlor-acetophenone under the anhydrous condition, then the intermediate condensates with papaverine forming the core pyrro[2,l-a]isoquinoline, followed by formation and lactonization to form the lactone ring. The second synthetic route uses prepared aldehyde with prepared ethyl nitroacetate by Knoevenagel condensation to obtain 2-Nitro-3-(2,4,5-tris-methoxy-phenyl)-acrylic acid ethyl ester and 2-Nitro-3-(2,4,5-tris-benzyloxy -phenyl)-acrylic acid ethyl ester etal intermediates. The lamellarin skeleton could arise from condensation of the papaverine and these intermediates by Michael reaction, the ester group is provided for subsequent lactonization. The third synthetic route uses coumarin or indan-l,3-dione derivatives and papaverine to form lamellarin under basic conditions.

第一条路线首先从1,2,4-三甲氧基苯出发与卤乙腈作用合成卤代芳酮中间体,然后与罂粟碱反应合成开链片螺素,最后经乙酰化、去保护、成内酯环得到片螺素;第二条路线由制备的芳醛和制备的硝基乙酸乙酯经缩合得到2-硝基-3-芳基丙烯酸乙酯,然后由该中间体与罂粟碱反应,在完成关环的同时也引入酯基,最后去保护、成内酯环得到片螺素;第三条路线是由香豆素或茚二酮出发,经溴代后的中间体与罂粟碱反应,得到片螺素的基本框架。

The famciclovir was synthesized from purine by a series of steps by Acylation, Decarboxylation, Reduction ,and so on; Derivatives of these intermediates is described from the 6-chloro- 9H- purin-2-amine as raw materials in different conditions when the iodine and bromide were synthesized with the addition of two intermediate 6-bromo-9H-purin-2-amine and 6-iodo-9H-purin-2-amine; There is elaborated from the main part of a acetophenone, urineaminohydrochloride, phenylhydrazine, ethyl acetoacetate as raw material through a series of reactions to synthetic 3-phenyl-4-formylphenyl pyrazole and 5-chloro-3-methyl-1-phenyl-1H-pyrazole-4-aldehyde two pyrazole aldehyde, and then with 2-amino-6-chlorine-9-(2-methicillin-oxo-co-methyl-4-yl) purine reaction of the two new pyrazole purine Schiff bases.

本论文主是采用以鸟嘌呤为原料,经过一系列的酰基化,脱羧,还原等反应作用下最终得到了产物2-氨基-9-(4-乙酰氧基-3-乙酰氧基甲基丁基)嘌呤;其中的中间体衍生物主要是阐述从以2-氨基-6-氯鸟嘌呤为原料通过在不同的条件下进行溴代与碘代分别合成了另外两种中间体2-氨基-6-溴鸟嘌呤及2-氨基-6-碘鸟嘌呤;还有一部分主要是阐述从以苯乙酮,盐酸氨基脲,苯肼,乙酰乙酸乙酯为原料通过一系列的反应先合成3-苯基-4-醛基吡唑及5-氯-3-甲基-1-苯基-1H-吡唑-4-甲醛这两个吡唑醛,然后再与2-氨基-6-氯-9-(2-甲氧羰基丁酸甲酯-4-基)嘌呤反应得到了两个新型的吡唑嘌呤席夫碱

Bromo-2-sulfolene (2) reacted with substituted benzoic acid salt s 3a~3c or alizarin yellow (3d) to give four novel allylic substitution products 4a~4d by esterification reaction, respectively.

以3,4-二溴环戊砜(1)为原料,在无水吡啶作用下发生消除反应,得到反应中间体4-溴-2-环戊烯砜(2),再分别与一系列取代苯甲酸盐3a~3c以及茜素黄GG(3d)发生酯化反应,合成出4种新环戊烯砜衍生物4a~4d,并用IR,1HNMR,MS,元素分析等表征了它们的结构。

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