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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。

Based on the detailed analysis of a variety of factors affecting stability of taxol production in Taxus cells, it was discovered that initial cell density and the relevant concentrations of substrates, elicitors and precursors significantly affected stability of taxol production; farther study showed that addition of elicitors at appropriate cellular state was the key to steadily improve taxol yield, especially, the proper cellular state was at the end of lag phase and at the beginning of the stationary phase, which was also proved by the cellular ultrastructure.

对影响红豆杉细胞紫杉醇产量稳定性的各类因素进行详细分析,发现细胞的接种密度以及与之相适应的培养基的基质浓度、诱导子浓度和前体浓度是影响紫杉醇产量稳定的重要因素;进一步研究发现,选择细胞处于合适的状态时加入诱导子是稳定提高紫杉醇产量的关键,细胞合适状态特别是延迟期末和稳定期初最合适,细胞状态的超微结构观察结果也证明了这一点;同时研究发现采用合适的同步化处理获得的细胞初始周期时相加入诱导子与紫杉醇产量稳定密切相关,且以低温同步化处理得到的细胞周期的分裂中期相的细胞加入诱导子不仅大大提高了紫杉醇的产量,而且诱导子加入时间大大缩短,有利于大大提高紫杉醇生产率。

Two kinds of polyaspartic acid derivates, i.e. PEG-g-PAsp and PEG-g-PDEA, were prepared through the ring-opening reaction of polysuccinimide by CH3O-PEG-NH2, followed by alkaline hydrolysis and aminolysis, respectively.

通过胺端基聚乙二醇(CH3O-PEG-NH2)开环聚琥珀酰亚胺,进一步碱解和胺解制备了聚乙二醇接枝聚天冬氨酸和聚乙二醇接枝聚乙二胺基天冬酰胺两种聚天冬氨酸衍生物。

Sixteen compounds were separated from 80% ethanol extract of Plant A, they were:-lariciresinol,-isolariciresinol,-isolariciresinol 9-O-β-D-glucopyranoside, tanegoside B, apiginin, apigenin 7-O-β-D-glucoside, apigenin 7-O-β-neospheroside, quercetin 3-O-β-D-glucopyranoside, 1, 7-dihydroxy-3, 4-dimethoxyxanthone, 3-O- [α-L-rhamnopyranosyl (1-4 ] -β-D-glucopyranoside-(25S)-5β-spirostan-3β-ol , 3β-O-D-glucopyranoside quinovic acid, mangiferin , 3'-p-hydroxybenzoyl-mangiferin, physcion, benzenyl methanol β-D-glucopyranoside and Vanillic acid.

结果: 1。从植物A的80%乙醇提取物中共分离得到16个化合物,分别为:-落叶松脂醇、-异落叶松脂醇、异落叶松脂醇9-O-β-D-吡喃葡萄糖苷、tanegoside B、芹菜素、芹菜素7-O-β-葡萄糖苷、芹菜素7-O-β-新橙皮糖苷、槲皮素3-O-β-D-吡喃葡萄糖苷、1,7-二羟基-3,4-二甲氧基-口山酮、菝葜皂苷元-3-O-[α-L-吡喃鼠李糖基(1-4)]-β-D-吡喃葡萄糖苷、喹诺酸3β-O-D-葡萄糖苷、知母宁、3′-对羟基苯甲酸-知母宁、大黄素甲醚、苯甲醇-β-D-吡喃葡萄糖苷、香草酸。

RESULTS: Sixteen compounds, ursolic acid (1), indole-3-carboxaldehyde (2), indole-3-carboxylic acid (3), p-coumaric acid (4), azelaic acid (5), N-trans-feruloyl tyramine (6), blumenol A (7), 2-hydroxy-3-methylanthraquinone (8), rubiadin l-methyl ether (9), rubiadin (10), quercetin (11), luteolin (12), chrysoeriol 6-C-β-boivinopyranosyl-7-O-β-glucopyranoside (13), alternanthin (14), stigmasta-5, 22-dien-3β-ol (15), and α-spinasterol (16) were obtained from the EtOAc extract of Alternanthera philoxeroides.

结果:得到并鉴定了16个化合物,分别为乌苏酸(1)、吲哚-3-甲醛(2)、吲哚-3-甲酸(3)、对-香豆酸(4)、壬二酸(5)、N-反式阿魏酰基酪胺(6)、布卢姆醇A(7)、2-羟基-3-甲基蒽醌(8)、甲基异茜草素-1-甲醚(9)、甲基异茜草素(10)、槲皮素(11)、木犀草素(12)、柯伊利素-6-C-β-波伊文糖基-7-O-β-吡喃葡萄糖苷(13)、莲子草素(14)、豆甾醇(15)和α-菠甾醇(16)。

DBP and DEHP have the similar photodegradation mechanism. The predominant pathway for DBP and DEHP photodegradation in the Fe -oxalate complexes system is hydroxyl radical extracting H atom in α-position of the aliphatic chain close to the carboxyl group followed by oxidation to produce alcoholized derivatives ROH. ROH then breaks down to phthalic acid and dialcohol that will be further oxidized up to mineralization.

DBP和DEHP的光降解历程相似,主要反应途径是OH自由基提取烷基上与羧基相连的α-H原子,然后被氧化生成醇衍生物,再分解成为酞酸和二醇,酞酸经历开环和进一步脱羧,二醇可以被氧化成为低级烷基羧酸,直至矿化。

Ingredients: Water,Lauric Acid,Myristic Acid,Stearic Acid,Propylene Glocol,Potassium Hydroxide,Cocamidopropyl Betaine,Starch Hydroxypropyltrimnium Chloride,Sodium Laureth Sulfate,Glycol Distearate,Lavandula Angustifolia Oil,Creatine,Tetrasodium Edta,Perfume,Dmdm Hydantoin.

成分: 去离子水,月桂酸,肉豆蔻酸,硬脂酸,丙二醇,氢氧化钾,椰油酰胺丙基甜菜碱,淀粉羟丙基三甲基氯化铵,月桂醇聚醚硫酸钠,乙二醇双硬脂酸酯,薰衣草精油,肌酸,乙二胺四乙酸四钠,香精,DMDM 乙内酰脲。

Based on relative literatures,this part has included five resesearch aspects as below.1 Fifteen compounds were isolated and purified by extraction,column chromatography,and their structures were determined on the basis of spectral analysis: acteoside(Ⅰ-1),isoacteoside(Ⅰ-2),crenatoside(Ⅰ-3),cistanoside F(Ⅰ-4),sinapoyl-4-O-β-D-glucoside(Ⅰ-5),adenosine(Ⅰ-6),β-siterol(Ⅰ-7),oleanic acid(Ⅰ-8), succinic acid(Ⅰ-9),caffeic acid(Ⅰ-10),protocatechuic aldehyde(Ⅰ-11),p-hydro xybenzyl alcohol(Ⅰ-12),β-daucosterol(Ⅰ-13),D-galacitol(Ⅰ-14),D-mannitol(Ⅰ-15).Ⅰ-4~15 were obtained from this plant for the first time,andⅠ-6,7,9,and 13 were isolated from Orobanche genus for the first time.2 The scavenging test of DPPH showed that most compounds have comparative antioxidant activity as L-ascorbic acid and part of them show better activity such as the O.coerulescens extract and phenylethanoid glycosides.Acteoside showed potent free radical scavenging effects with a median inhibition concentration of 25.6μg/ml.3 The anti-HBV activities of acteoside,isoacteoside and crenatoside were measured,and all of them showed suppressive activity on the expression of HBsAg and HBeAg in the HepG2.2.15 cell line.

本论文在文献调研基础上对紫花列当化学成分及生物活性进行了研究,并从免疫抗病毒角度探讨紫花列当中特征性成分类叶升麻苷的肝保护作用及其机制。1采用大孔树脂、硅胶和Sephadex LH-20等色谱技术对紫花列当进行系统的植物化学研究,从中分离得到19个化合物,利用UV和NMR等波谱手段及理化性质鉴定了其中的15个化合物,分别为类叶升麻苷(Ⅰ-1)、异类叶升麻苷(Ⅰ-2)、crenatoside(Ⅰ-3)、cistanoside F(Ⅰ-4)、sinapoyl-4-O-β-D-glucoside(Ⅰ-5)、腺苷(Ⅰ-6)、β-谷甾醇(Ⅰ-7)、齐墩果酸(Ⅰ-8)、琥珀酸(Ⅰ-9)、咖啡酸(Ⅰ-10)、原儿茶醛(Ⅰ-11)、对羟甲基苯甲酸(Ⅰ-12)、β-胡萝卜苷(Ⅰ-13)、D-半乳糖醇(Ⅰ-14)和甘露醇(Ⅰ-15除化合物Ⅰ-1、Ⅰ-2和Ⅰ-3外,其余化合物均为首次从该植物中分离得到。2)通过大孔树脂富集该药材有效部位苯乙醇总苷,并采用HPLC测得其所含特征性成分类叶升麻苷的含量可达80%以上。3DPPH自由基清除试验显示紫花列当提取物及其所含的苯乙醇苷类化合物均具有较好的抗氧化能力,其清除DPPH自由基能力接近于抗坏血酸。4采用卡介苗整体致敏、脂多糖离体攻击构建大鼠原代肝细胞免疫性损伤模型,在体外观察类叶升麻苷的保肝作用。

Chiral 3 methy 1,4 butanediol and its derivatives are the important intermediate of synthesis of chiral smectic liquid crystal polyesters and chiral natrual products with biological activity. In the paper, a new efficient route of 3 methyl 1,4 butanediol and its two derivatives, 2 methyl 4 tetrapyranyloxy 1 butanol and 2 methyl 4 tetrapyranylbutanal, was described, and the target products were synthesized by employing asymmetric hydroboration oxidation improved.

手性2-甲基-1,4-丁二醇及其衍生物是合成各种手性近晶型液晶材料以及手性天然生物活性物质的重要中间体,以3-甲基-3-丁烯-1-醇为原料利用改进的不对称硼氢化-氧化反应,成功地合成了-2-甲基-1,4-丁二醇以及其2种手性衍生物:-2-甲基-4-四氢吡喃氧基-1-醇和-2-甲基-4-四氢吡喃氧基丁醛。

Plant polyprenols, which have similar structure and biological activity to dolichols in human body, are lipids of polymer with isoprenyl units. However, dolichols are key carriers in biosynthesis process of glycosyl derivatives with protein.

植物聚戊烯醇是一类异戊烯基结构聚合体的类脂化合物,与人体内多萜醇具有相似的结构特征和生理活性,而多萜醇是糖基与蛋白质生物合成的关键载体。

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