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A series of novel dendrons with 1,3,5-triazine structure were synthesized by convergent strategy using cyanuric chloride, p-hydroxyazobenzene,β-naphthol, 1-hydroxyanthraquinone, 3,5-dihydroxybenzyl. They were the first generation p-phenyl-azo-phenyloxy-terminated dendron G1.0, the first generation naphthyloxy-terminated dendron G1.0, the first generation naphthyloxy-terminated and 1-anthraquinonoxy-cored dendron G, and the second generation naphthyloxy-terminated dendron G2.0.

以对羟基偶氮苯、β-萘酚为端基,三聚氯氰、3,5-二羟基苄醇为支化单体,1-羟基蒽醌为核心,用收敛法合成了一系列新型结构的含均三嗪环的树枝块:第一代端基为偶氮苯的树枝块G1.0、端基为萘氧基的树枝块G1.0、端基为萘氧基、中心为蒽醌的树枝块G、第二代端基为萘氧基的树枝块G2.0。

In a system consisting of 20% PEG 400 and 12% magnesium sulfate, the partition coefficient of PGA was less than 0.01, PGA almost completely partitioned into the magnesium sulfate-rich bottom phase. Meanwhile, the partition coefficient of cephalexin was 6.7, the partition coefficients of phenylglycine methyl ester and 7-ADCA were 1.5 and 1.2, respectively.

通过考察头孢氨苄、苯甘氨酸甲酯和7-氨基脱乙酰氧基头孢烷酸(7-ADCA)在ATPS中的分配行为建立了一个含20%PEG 400和12%硫酸镁的ATPS,在此体系中头孢氨苄的分配系数为6.7,苯甘氨酸甲酯的分配系数为1.5,7-ADCA的分配系数为1.2,且青霉素酰化酶的分配系数小於0.01。

Chapter three: The studies of zinc dust assisted the green carbonyl olefination under thesolvent-free conditions.

第三章:锌粉促进无溶剂下羰基化合物的绿色烯基化反应研究该部分首次研究了在TMSiCl存在下,无溶剂非催化条件下,锌粉促进溴化苄与羰基化合物的烯基化反应,发现在无溶剂锌粉促进下,可以将羰基化合物立体选择性

Preparation of the lateral chain-4-benzyloxy-3-hydroxy butyronitrile is introduced as the substrate, the REFORMATSKY reaction is performed, then obtains the dicarbonyl ester, in the structure of which containing a chiral hydroxyl group, then performs the chiral reduction, take off the benzyl group after the protection reaction with acetonylidene,then obtains the lateral chain by oxidation.

手性侧链醛的合成:采用-4-苄氧基-3-羟基丁腈作为底物,通过REFORMATSKY反应缩合得到含有手性羟基的二羰物酯,再手性还原,丙酮叉保护后氢解脱苄,最后氧化得到侧链醛。

Results Compound albicanyl caffeate displayed strong antifungal property with MIC 4 μg/ml, while moderate antifungal effects (MIC16 μg/ml)were observed with compounds emodin, resveratrol, 3,4'-difluorostilbene, 2,2'-difluorostilbene and 2,3',5'-trifluorostilbene. Pakyonol, catechin, ampelopsin A, 3,4,4'-trihydroxyl- bibenzyl, 2,4'-difluorostilbene, 4-fluorostilbene,2-methyloxy-4'-fluorostilbene showed lower activity with MIC 32 μ g/ml.

结果化合物albicanyl caffeate对白色念珠菌表现出强的抗真菌活性,MIC为4μg/ml;而化合物大黄素、白藜芦醇、3,4'-二氟二苯乙烯、2,2'-二氟二苯乙烯及2,3',5'-三氟二苯乙烯显示出中等程度的抗真菌活性,MIC为16μg/ml;双联苄pakyonol、多酚类儿茶素、白藜芦醇二聚体野葡萄素A、3,4,4'-三羟基联苄、2,4'-二氟二苯乙烯、4-氟二苯乙烯及2-甲氧基-4'-氟二苯乙烯显示出较弱的抗真菌活性,MIC为32 μg/ml。

Seven Schiff bases of N-(4-hydroxyphenylmethylene)-1-naphthylamine, N-(4-hydroxyphenylmethylene)-p-methoxyaniline, N-(4-hydroxyphenylmethylene)-benzylamine, N-(4-hydroxy-3-methoxyphenylmethylene) furfurylamine, N-(4-hydroxy-3-methoxyphenyl methylene)-p-methylaniline, N-(4-hydroxy-3-methoxyphenylmethylene)-p-methoxyaniline and N-salicylidene-4-aminoantipyrine were first synthesized by the one step solid phase reactions between aromatic aldehydes with phenolic hydroxyl and amines at room temperature without solvent.

分别以带酚羟基的芳醛与胺类反应,首次通过室温固相反应一步合成了N-(4-羟基苯基亚甲基)-1-萘胺、N-(4-羟基苯基亚甲基)-对甲氧基苯胺、N-(4-羟基苯基亚甲基)-苄胺、N-(4-羟基-3-甲氧基苯基亚甲基)糠胺、N-(4-羟基-3-甲氧基苯基亚甲基)-对甲苯胺、N-(4-羟基-3-甲氧基苯基亚甲基)-对甲氧基苯胺和N-亚水杨基-4-氨基安替比林7种Schiff碱,反应15min完成,产率均超过90%。

In order to study strcture-bioactivity relationship concerning α,β-unsaturated-γ-lactones, we further synthesized γ-benzyloxymethy-γ-butanolide XXIII and the corresponding unsaturated buteno- lido XXV Scheme 6, p.

为了研究该类化合物的构效关系,在本论文第三部分,我们进一步设计并合成了--γ-苄氧基甲基-γ-丁内酯XXIII和--γ-苄氧基甲基-γ-丁烯内酯XXV这两个内酯化合物,目的是想考察内酯的α,β-不饱和双键是否是产生细胞毒性的关键结构。

Two monomers,bispmpargyl ether of bisphenol-Aand 4,4'-biphenyl dibenzyl azide were synthesized and characterized with FT-IR,1H-NMR and elementary analysis.

合成了两种单体双酚A二炔丙基醚与4,4′-联苯二苄叠氮,研究了一种新的低温聚合体系——双酚A二炔丙基醚与4,4′-联苯二苄叠氮在烘箱中的本体聚合行为。

Tetrachloroterephthalic acid was prepared by chlorinating terephthalic acid, oleumsolvent and iodine catalyst. Tetrachloroterephthalic acid was acylated by sulphurous oxychloride in the presence of DMF to form tetrachloroterephthaloyl chloride. The acyl chloride product was fluorinated by potassium fluoride and esterified by methanol to synthesize dimethyl tetrafluoroterephthalate. The ester was reduced with potassium borohydride and lithium chloride to give tetrafluoroterephthalyl alcohol. The above product was bromated in the hydrobromic acid to obtain 4-bromomethyl-2,3,5,6-tetrafluoro-benzene methanol. 4-Methyl-2,3,5,-6-tetrafluorobenzene ethanol was obtained by reducing the bromide with magnesium. In the exist of DCC and DMAP, tefluthrin was got by the condensation reaction between 4-methyl-2,3,5,6-tetrafluoro-benzene methanol and-(1RS,3RS)- 3-(2- chloro-3,3,3-trifluoro-1-propenyl)-2,2-dimethyl cycolpropanecar-boxylate acid.

对苯二甲酸与氯气在碘存在下以发烟硫酸为溶剂进行氯化制备四氯对苯二甲酸;再以DMF为催化剂与二氯亚砜反应生成四氯对苯二甲酰氯;以氟化钾为氟化剂,环丁砜为溶剂置换氟化,再与甲醇酯化得到四氟对苯二甲酸甲酯;以KBH4-LiCl为还原剂二甲醚为溶剂反应制得四氟对苯二甲基苄醇;以氯苯为溶剂在溴化氢溶液中溴化得到溴化产物;在乙醇溶液中经镁粉还原得到4-甲基-2,3,5,6-四氟苄醇;甲基苄醇与功夫酸在催化剂二环己基碳二亚胺和4-二甲氨基吡啶作用下缩合得到七氟菊酯,总收率达43.6%。

All of the tripodal schiff base ligands and their complexes were characterized.

以三乙醇胺、巯基苯胺、巯基乙胺为初始原料,设计合成了六个三脚架结构的化合物,其合成路线如下:三乙醇胺与氯化亚砜反应得到三(2-氯乙基)胺(1),然后与巯基苯胺或巯基乙胺在碱性条件下反应生成三脚架结构的三{[2-(2-氨基苯基)硫代]乙基}胺(2)或三{[2-(2-氨基乙基)硫代]乙基}胺(3),然后再与水杨醛、2-甲酰基-8-羟基喹啉(8)、2-甲酰基-8-苄氧基喹啉(7)反应得到六种新型的含硫西佛碱化合

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Detailed Intrinsic Reaction Coordination calculations were carried out to guarantee the optimized transition-state structures being connected to the related tautomers.

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