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氨基化合物

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Then Doripenem came into the market in the July ,2005. We studied the synthesis of Doripemen.Firstly, we synthesized the chemical 2 from the starting material------o-hydroxylphenylacylamine through Reformastky reaction, alkylation, Diekmann reaction, enolization, esterification and etc. Secondly, we synthesized the chemical 3 from L — hydroxylproline through the protection of carboxyl, amidogen and hydroxyl group, reduction by NaBr, SN_2 substitution and Mitsumobu reaction.

我们以水杨酰胺为起始原料,经Reformatsky反应、烷基化、Diekmann环合、烯醇化、酯化等反应合成双环母核2;再从L-羟基脯氨酸出发,经酯化保护羧基、保护氨基、保护羟基、硼氢化还原酯得醇、Sn2取代和Mitsumobu反应等合成巯基侧链3;最后由化合物3经脱保护、水解得硫醇,和化合物2在二异丙基乙基胺的作用下缩合,最后Pd/C催化脱保护,历经16步反应最终得到产物多尼培南。

In this paper, we designed and synthesized a molecule of compound 1, 2-(benzooxazol-2-yl)-5-4-(3-(benzothiazol-2-yl) phenylamino-6--1,3,5-triazin-2-ylaminophenol, which can only assembled into an organogel upon a short irradiation with ultrasound in toluene-methanol mixed solvent. DSC, XRD and IR were used to detect the properties and mechanisms of the organogel.

本论文中,我们设计合成了一个有机小分子化合物1,4-氨基(2-羟基苯基)苯并噁唑3-氨基苯基苯并噻唑二辛基胺缩三聚氯嗪,研究发现,在甲苯/甲醇=1:2的混合溶剂中,只有利用超声才能使之形成凝胶,加热冷却的方法不能形成凝胶,而形成针状结晶。

Two novel pyrazolone derivatives 2-ethylamino-6H-5-(1-phenyl-3-methyl/phenyl-5-pyrazolone-4-ylene)-1,3,4-thiadiazine (PMCP-ETSC/DPCP-ETSC) containing NNS six-membered heterocycles were synthesized by the condensation reaction of 1-phenyl-3-methyl/phenyl-4-chloroacetyl-pyrazolone-5 with 4-ethyithiosemicarbazide. The title compounds were characterized by elemental analysis, IR, 1H NMR, 13C NMR and single-crystal X-ray diffraction.

利用1-苯基-3-甲基/苯基-4-氯乙酰基-吡唑啉酮-5与4-乙基氨基硫脲发生缩合反应,生成了2个新的双杂环化合物2-乙氨基-6H-5-(1-苯基-3-甲基/苯基-5-吡唑啉酮-4-基)-1,3,4-噻二嗪(PMCP-ETSC/DPCP-ETSC),并对其进行元素分析、红外光谱、核磁共振表征和晶体结构分析。

The a-amino groups of amino acids react reversibly with aldehydes to form a variety of compounds, each of which is called a Schiff's base.

氨基的α氨基与醛反应是可逆的,可形成多种化合物,每一种都叫希夫碱。

On the basis of previous work in our laboratory, several novel thiosemicarbazones and semicarbazone compounds containing pyrazolone-ring have been synthesized.

本文在实验室原有工作的基础上,合成了以吡唑啉酮环为变色主体的缩氨基脲、氨基硫脲类有机光致变色化合物,通过对固态光致变色性质和晶体结构的研究,深入分析了它们的变色机理,并总结了光致变色性质与之间结构的关系。

The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9-; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is -C-,-O-C-,-NR8-C-,-O-C1-6alkanediyl-C-,-NR8-C1-6alkanediyl-C-,-S2-,-O-S2-,-NR8-S2 ; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC, carboxyl, aminoC, mono- or di(C1-4alkyl)aminoC, C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; R5 and R6 are H or C1-6alkyl.

本发明涉及右式化合物其N-氧化物、盐、立体异构形式、外消旋混合物、前药、酯及代谢物,其中R 1 及R 8 各是氢、C 1-6 烷基、C 2-6 烯基、C 3-7 环烷基、芳基、Het 1 、Het 2 ;R 1 也可以是式(R 11a R 11b )NC(R 10A R 10b )CR 9 -之基;t是0、1或2;R 2 是氢或C 1-6 烷基;L是-C-、-O-C-、-NR 8 -C-、-O-C 1-6 烷二基-C-、-NR 8 -C 1-6 烷二基-C-、-S 2 -,-O-S 2 -、-NR 8 -S 2 -;R 3 是C 1-6 烷基、芳基、C 3-7 环烷基、C 3-7 环烷基C 1-4 烷基或芳基C 1-4 烷基;R 4 是氢、C 1-4 烷基OC、羧基、氨基C、一-或二(C 1-4 烷基)氨基C、C 3-7 环烷基、C 2-6 烯基、C 2-6 炔基或任选被取代的C 1-6 烷基;R 5 及R 6 是氢或C 1-6 烷基。

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

Owing to different structures of cotton fiber and chitin fiber ,they have different adsorbability to reactive dyestuffs.

采用不同的醛类化合物对甲壳素纤维上的氨基进行保护,活性染料染色后用稀酸脱去氨基的保护基。

With TEMPO(5 mol%) as the catalyst,N-methyl-N-phenyl-hydrazine(1.2 equiv.) as the amine source,the direct ortho-amination of 2-naphthols could be easily achieved.The reaction was carried out at room temperature under air atmosphere.

以5 mol%TEMPO为催化剂,1.2当量N-甲基-N-苯基肼作氨源,二氯甲烷为溶剂,空气中,室温下,实现了对2-萘酚邻位氨基化,可以高效的合成1-氨基-2-萘酚类化合物。

With TEMPO(5 mol%) as the catalyst,N-methyl-N-phenyl-hydrazine(1.2 equiv.) as the amine source,the direct ortho-amination of 2-naphthols could be easily achieved.

以5 mol%TEMPO为催化剂,1.2当量N-甲基-N-苯基肼作氨源,二氯甲烷为溶剂,空气中,室温下,实现了对2-萘酚邻位氨基化,可以高效的合成1-氨基-2-萘酚类化合物。

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