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Odoquinazolin-4(3H)-one,7-methyl-4(3H)-quinazolinone,7-bromoquinazolin-4(3H)-one were synthesized by using anthranilic acid、2-amino-5-nitrobenzoic acid、2-amino-4-nitrobenzoic acid,6-nitro--4(3H)-quinazoline-one、o-amino-terephthalic acid, 2-amino-4-hydroxy benzoic acid、2-amino-5-bromo-benzoic acid、2-amino-5-iodine acid,1、4-butynediol、L-glutamine、isatin anhydride、formamide as starting materials and utilizing microwave-assisted synthetic approach.

本文利用微波辅助合成的方法,以邻氨基苯甲酸、2-氨基-5-硝基苯甲酸、2-氨基-4-硝基苯甲酸、邻氨基对苯二甲酸、2-氨基-4-羟基苯甲酸、2-氨基-5-溴苯甲酸、2-氨基-5-碘苯甲酸、5-甲基-2-氨基苯甲酸等为原料与甲酰胺反应,以及以1,4-丁炔二醇、L-谷氨酰胺与靛红酸酐反应,共合成了13个喹唑啉酮衍生。。。

Methods: In this paper, a quinazoline purine analogues for the parent nucleus, respectively, and four of its seven introduced to replace the structure of diverse and flexible side-chain amino-benzene, design a series of 4 - to replace the aniline-based -6 - methoxy --7 -(2 - hydroxy replace C oxy) quinazoline compounds.

目的:通过各种化学合成方法完成目标化合物4--6-甲氧基-7-(2-羟基取代丙氧基)喹唑啉的合成并对目标化合物进行结构修饰,以期获得高活性的表皮生长因子受体酪氨酸激酶抑制剂。

Objective: through various chemical synthesis target compounds 4 -- 6 - the - 7 -(2 - hydroxyl replace c oxygen radicals) quinazoline compounds were synthesized and the structure of the modified, so as to get high epidermal growth factor receptor tyrosine kinase inhibitor.

目的:通过各种化学合成方法完成目标化合物4--6-甲氧基-7-(2-羟基取代丙氧基)喹唑啉的合成并对目标化合物进行结构修饰,以期获得高活性的表皮生长因子受体酪氨酸激酶抑制剂。

the target compounds synthesized to synthesize a series after 4 - instead of aniline - 6 -(2 - hydroxyl replace c oxygen radicals) quinazoline compounds has laid a good foundation.

目标化合物的顺利合成为以后合成一系列4-取代苯胺-6-(2-羟基取代丙氧基)喹唑啉类化合物奠定了良好的基础。

The goal of the successful synthesis of compounds for the subsequent synthesis of a series of 4 - to replace the aniline -6 -(2 - hydroxy replace C oxy) quinazoline compounds laid a good foundation.

目标化合物的顺利合成为以后合成一系列4-取代苯胺-6-(2-羟基取代丙氧基)喹唑啉类化合物奠定了良好的基础。

According to the result, we believed that the reason resulted in the low sensitivity was that the marker residue compound MQCA structure has changed after conjugated with protein and the antibody induced by the conjugation could not recognize the free MQCA in the ci-ELISA. Therefore we designed some hapten which could reserve the marker residue structural speciality mostly. After synthesis route selection and optimum, the hapten 7-Hydroxymethyl-3-methyl-quinoxaline-2-carboxylic acid was synthesized, used 4-methyl-2-nitroaniline as the start material via six steps, such as oxidation cyclization, bromize reaction, hydrolysis, Beirut reaction, reduction, hydrolysis. This work established basis for producing the high affinity antibody and developing the sensitive ELISA residue detection method.

本论文认为导致ELISA检测灵敏度较低的原因,是残留标示物和蛋白偶联后的特征结构发生改变,诱导产生的抗体不能够对游离MQCA很好的识别,因此,本论文设计了能够最大化保留MQCA结构特征的系列半抗原结构,并对其合成路线进行了筛选和优化,最终以对甲基邻硝基苯胺为起始原料,经氧化环化、溴代、水解、Beirut缩合、还原、水解六步反应制备含羟甲基结构的MQCA衍生物7-羟基甲基-3-甲基-喹噁啉-2-羧酸,为制备对游离残留标示物高亲和力的抗体,高灵敏度的ELISA残留检测方法的建立奠定基础。

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