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The results of clinical assessment showed that levosimendan was safe and effective which could improve the prognosis of the patients and kept normal blood kinetics. By improving the reported synthetic route, levosimendan was synthesized from acetanilide via eight steps of reaction.

本论文探索了左西孟旦的合成路线,对文献报道的合成工艺进行了合理有效的改进,以乙酰苯胺为原料,最终经Friedel-Crafts反应,羰基α-位溴代,丙二酸二乙酯缩合,水解,脱羧,环合,拆分及重氮化加成等八步反应合成了左西孟旦。

Study on the Crystallization Process of Labeled GL-7-ACA Acylase CA130 Complex 7β-bromoacetyl amino cephalosporanic acid (BA-7-ACA), an analog of glutaryl-7-amino cephalosporanic acid (GL-7-ACA), can inhibit and specifically alkylate GL-7-ACA acylase (CA130) from Pseudomonas sp. 130, forming a carbon-carbon bond between BA-7-ACA and the C-2 on indole ring of Trp-β4 residue of CA130.Here we reported that BA-7-ACA labeled CA130 (BA-C130) could self-catalyze the hydrolysis of BA-7-ACA during crystallization process. The hydrolysis was confirmed to be a reaction analogous to the one of GL-7-ACA by comparative MALDI-TOF (matrix-assisted laser desorption/ionization-time of flight) spectrometry analysis.

二、GL-7-AcA酰化酶CA130标记复合物的结晶过程研究溴乙酰氨基头孢烷酸(7β-bromoacetyl amino cephalosporanic acid,BA-7-ACA)作为戊二酰-7-氨基头孢烷酸(GL-7-ACA)的类似物,不仅能够抑制GL-7-ACA酰化酶CA130的活力,而且能通过在BA-7-ACA和CA130的β亚基第四位色氨酸吲哚环二位碳原子之间形成碳-碳共价键而将CA130特异的烷基化。

So the ester type cinchona alkaloid derivatives should be the preferable catalysts for the IFB reaction withβ-phenyl substituted bromoketones as substrate.

由此可知,这类以酯键形成的金鸡纳生物碱衍生物适于催化β-苯取代溴乙酰甲酸乙酯为底物的IFB反应。

Ib was synthesized by condensation of phthalic anhydride with 2-methylresorcinol in fused AlCl〓/NaCl (5∶1), followed by selective acetylation, methylation, NBS bromination and condensation with sodium ethoxide.

邻苯二甲酸酐在熔融的三氯化铝-氯化钠(5:1)中和-2,6-二羟基甲苯环合得1,3-二羟基-2-甲基蒽醌〓后经选择性乙酰化、甲基化、NBS溴化、乙醇钠缩合得1-甲氧基-2-乙氧甲基-3-羟基蒽醌。

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 intermediate which obtained from oximation of 7a-e reacted withmethyl N-(2-bromomethylphenyl)-N-methoxycarbamate to synthesize oxime ether methyl carbamate 3a-e.

以邻位卤代苯甲醛和3-丁烯-2-醇为原料通过钯催化&一锅法&反应合成了2-乙酰基茚7a-e,7a-e 肟化之后和N-(2-溴甲基苯基)-N-甲氧基氨基甲酸甲酯反应合成了肟醚类氨基甲酸甲酯3a-e,进一步胺解之后得到了肟醚类氨基甲酰甲胺3f-j。

In our work, as a preliminary experiment, the N-phenacylisoquinolinium bromide was reacted with methlhydrazine in refluxed acetic acid. Unexpectedly, 2-methyl-1,2,3-triazole was obtained. The further study of this reaction led to a more simple starting material,α-bromoacetophenone to react with methylhydrazine, obtaining the same product.

我们在研究N-苯乙酰异喹啉溴化物与甲肼在冰醋酸中的反应时,意外地得到了2-甲基-4-苯基-1,2,3-三氮唑,经过进一步的研究发现α-溴代苯乙酮与甲肼也能得到同样的产物。

A HPLC method for determination of phenylephrine hydrochloride, paracetamol, caffeine anhydrous ,salicylamide and brompheniramine maleate in Liufenkamin tablets was established.

建立了HPLC法测定柳酚咖敏片中盐酸去氧肾上腺素、对乙酰氨基酚、无水咖啡因、水杨酰胺、马来酸溴苯那敏的含量。

Four substances including 2-methyl ethyl acetoacetate and barley straw extract distilled from bulrush as well as cetyl trimethyl ammonium bromide and isothiazo lintone were used for the comparison experiment in inhibiting the growth of Microcystis aeruginosa in various phases. Result showed that inputting chemicals in the lag phase has better effect than in the log phase, and adding in lag phase can effectively inhibit the algae growth. Although feeding allelopathic substance at log phase can lead to certain restraining effect, it cannot result in the effective inhibition of algae growth, which can be well achieved by feeding CTAB and isothiazo lintone below 10mgl/L during log phase.

研究用从芦苇中提取的2-甲基乙酰乙酸乙酯和大麦秸浸出液两种化感物质以及十六烷基溴化钱和异噻唑啉酮等四种药剂对不同生长期的铜绿微囊藻进行了对比抑制试验,结果显示在铜绿微囊藻生长的迟缓期投加试验药剂效果比在对数期投加效果都好,在迟缓期投加四种药剂,都有很好的抑藻效果;在铜绿微囊藻生长的对数期投加化感物质,虽然有一定的抑藻率,但效果较差,而在藻对数期投加10mg/L以下的CTAB和异噻唑啉酮能达到很好的水华抑制效果。

Benzoyl chloride, phthaloyl dichloride, isophthaloyl dichloride and terephthaloyl dichloride were reacted with cinchona alkaloids to form 16 esters type catalysts 4a-d, 5a-d, 6a-d and 7a-d.

1对于溴乙酰甲酸乙酯为底物的反应,这类以酯键形成的金鸡纳生物碱衍生物表现出的不对称诱导作用不令人满意(22-75%ee)。

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According to the clear water experiment, aeration performance of the new equipment is good with high total oxygen transfer coefficient and oxygen utilization ratio.

曝气设备的动力效率在叶轮转速为120rpm~150rpm时取得最大值,此时氧利用率和充氧能力也具有较高值。

The environmental stability of that world - including its crushing pressures and icy darkness - means that some of its most famous inhabitants have survived for eons as evolutionary throwbacks, their bodies undergoing little change.

稳定的海底环境─包括能把人压扁的压力和冰冷的黑暗─意谓海底某些最知名的栖居生物已以演化返祖的样态活了万世,形体几无变化。

When I was in school, the rabbi explained everythingin the Bible two different ways.

当我上学的时候,老师解释《圣经》用两种不同的方法。