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Started from D-tyrosine, we obtained the tetramic acid 96 using Jouin reaction. The assembly of the second fragment 109 was stared from 1,4-butandiol,using asymmetric alkylation reaction developed by Oppolzer as a key step. Coupling of the tetramic acid 96 with 109 provided the key intermediate 110 according to Yoshii\'s procedure. After remove protective group and Sharpless epoxidation, we obtained the key intermediate 113. Its macrocyclization to form the final product is in progress.

本论文的第二章主要对Macrocidin A开展了合成工作,我们从D构型的酪氨酸出发,经过官能团转换;利用Jouin反应生成Tetramic acid 96,另外一个片断从1,4-丁二醇开始经过多步反应生成碘化物104,利用Oppolzer发展的手性樟脑磺酰胺为辅基参与的不对称烷基化反应,引入手性甲基,生成关键中间体109,接着通过Yoshii发展的方法连接96和109生成110,经过Sharpless不对称环氧化反应建立环氧化合物,然后脱去保护基得到关环前体113,分子内的Mitsunobu反应进行关大环反应正在进行之中。

Acylamino compounds from AD were synthesized by cleavage of A-ring through NaIO4/KMnO4 oxidation, ring closure by amination, oximation with hydroxylaminechloride in C-17 position, and reduction of oxime in C-17 position and substitution with substituted acylchloride and carboxylic acids.

本文以AD为起始原料,经过NaIO4/KMnO4氧化裂解、胺解环合、羟氨肟化反应,在甾体17位形成肟,并将肟还原成胺,与取代酰氯和有机羧酸反应,合成了15个酰胺化合物。

Synthesized three new dithiocarbohydrazones: 1, 5-bis (4-methoxybenzaldehyde) dithiocarbohydrazone (1), 1, 5-bis (p-dimethyl aminobenzaldehyde) dithiocarbohydrazone (2), 1, 5-bis (2-furaldehyde) dithiocarbohydrazone (3), and initially reported the 〓C NMR data of the dithiocarbohydrazones.

合成了3—(谷氨酮—1—基)—4—氨基—5—巯基—1,2,4—均三唑新的中间体化合物,以元素分析,IR,NMR,MS实验技术对其结构进行了表征,研究其NMR波谱特征,并以〓H-〓H COSY,〓C-〓H COSY,COLOC二维NMR技术对其〓H,〓C NMR的谱峰进行了全归属。

METHODSThe compounds were prepared by using 2ethylpyridine, through the Whol Ziegler reaction, the Williamson reaction and aminolysis. The effects for ability of memory in mice were measured by swimming maze test.

方法]以2乙基吡啶为原料,经WholZiegler反应、Williamson反应及氨解反应得到2[1(2吡啶)乙氧基]乙酰4取代哌嗪,采用水迷宫法观察所合成的化合物对小鼠记忆力的影响。

Methods Compound 3 was got via the formation of the amide from 2-chloro-3-amino-4-methyl pyridine and 2-chloronicotinoyl chloride, and then nevirapine was acquired by the aminolysis of 3 with cyclopropylamine in an autoclave, followed by the intramolecular nucleophilic substitution.

以2-氯-3-氨基-4-甲基吡啶为原料,依次与2-氯烟酰氯缩合成化合物3、再与环丙胺高压氨解、最后发生分子内亲核取代反应,成功合成了奈韦拉平。

A clean production technology for fluorine and silica white is introduced, with fluorine-containing gas raw material directly absorbed by ammonium fluoride, or ammonia to obtain ammonium fluorosilicate ,and to get ammonium fluoride and silica white by ammonization, further to manufacture other fluoride product with high value.

介绍一种利用磷肥生产中的含氟废气生产氟化合物与白炭黑的清洁生产方法:用氟化铵或氨直接吸收含氟气体生成氟硅酸铵,然后氨化得氟化铵与白炭黑(SiO2),氟化铵可进一步加工为其它高价值氟化物产品。

Bis-(2,3-dibromo-4,5-dihydroxy-phenyl)-methane is a natural bromophenol with significant inhibition against PTP1B IC_(50=2.4μmol/L, which was isolated from the ethanol extract of red algae Rhodomela confervoides.

双-(2,3-二溴-4,5-二羟基苯基)-甲烷是从松节藻醇提物中分离鉴定出的溴酚类化合物,体外活性筛选发现,它具有极强的蛋白酪氨酸磷酸酶1B(PTP1B)抑制活性IC_(50=2.4μmol/L。

Any of several esters, other than the ethyl ester, of carbamic acid .

亚胺源自氨的一种化合物,含有与一个二价非酸基结合的氨基

In order to mimic this repair process of apoenzyme, we synthesized two model compounds, in which tryptophan and/or tyrosine was covalently linked to cyclobutane thymine dimer, and measured the splitting quantum yield of dimer under 295 nm light. By investigating the photosensitized splitting properties of the dimer, some new insights into the intramolecular electron-transfer process were gained.

为了模拟酶蛋白的这一修复过程,合成了色氨酸和/或酪氨酸与胸腺嘧啶二聚体共价连接的化合物,作为酶-底物复合物的模型,研究了它们在295 nm光照射下氨基酸残基光敏化二聚体裂解的性质,测定了二聚体裂解量子产率,获得一些新的结果并对其进行了分析。

The key part of this project is the application of high effective degradative microorganisms for aromatic hydrocarbons and nitrify bacteria for biological nitrogen removal in the treatment of recalcitrant industrial wastewater.

本项目的关键技术是将人工筛选的芳香族化合物降解菌和生物脱氮的硝化细菌应用于难降解的工业废水处理工程。技术特点是:可在去除难降解有机物的同时脱除高浓度的氨氮。

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