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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。

Suitable water-immiscible organic solvents include aromatic hydrocarbons, eg toluene, xylene, naphthalene, tetrahydronaphthalene and methyl naphthalene; chlorinated aromatic hydrocarbons, eg chlorobenzene, fluorobenzene, chloronaphthalene and bromonaphthalene; esters, eg butyl acetate, ethyl acetate, methyl benzoate, ethyl benzoate, benzyl benzoate, butyl benzoate, phenylethyl acetate, butyl lactate, benzyl lactate, diethyleneglycol dipropionate, dimethyl phthalate, diethyl phthalate, dibutyl phthalate, di(2-ethylhexyl) phthalate; alcohols having six or more carbon atoms, eg hexanol, octanol, benzyl alcohol, phenyl ethanol, phenoxy ethanol, phenoxy propanol and phenoxy butanol; ethers having at least 5 carbon atoms, preferably C 5-14 ethers, eg anisole and phenetol; nitrocellulose, cellulose ether, cellulose acetate; low odour petroleum distillates; turpentine; white spirits; naphtha; isopropylbiphenyl; terpene; vegetable oil; mineral oil; essential oil; and natural oil; and mixtures of any two or more thereof.

适用于水互溶的有机溶剂包括芳香族碳氢化合物,如甲苯,二甲苯,萘,四氢萘和甲基萘;氯代芳香族碳氢化合物,如氯苯,氟,氯萘和萘;酯类,如醋酸丁酯,醋酸乙酯,苯甲酸甲酯,苯甲酸乙酯,苄酯,苯甲酸正丁酯,苯,醋酸丁酯乳酸,乳酸苄,二甘醇二丙酸酯,邻苯二甲酸二甲酯,邻苯二甲酸二乙酯,邻苯二甲酸二丁酯,二(2乙基己基)酯;醇有6个或更多碳原子,如己醇,辛醇,苯甲醇,苯乙醇,苯氧基乙醇,丙醇和苯氧基苯氧丁醇;醚至少有5个碳原子,最好荤5-14醚,如苯甲醚和phenetol;硝化棉,纤维素醚,醋酸纤维素,低气味石油蒸馏;松节油;白酒,石脑油isopropylbiphenyl;萜类,植物油,矿物油,挥发油;和天然油,以及任何两个或两个以上其混合物。

Calicheamicin can be conjugated to the non-specific antibody using a 4-(4'-acetylphenoxy) butanoic acid or (3-Acetylphenyl) acetic acid linker.

可使用4-(4′-乙酰基苯氧基)丁酸或(3-乙酰基苯基)乙酸连接子使卡奇霉素与所述非特异性抗体共轭结合。

Ozonation could not reduce TOC completely, the results of HPLC and GC-MS showed that p -CNB was mainly transformed into p -chlorophenol, p -nitrophenol, 2-chloro-5-nitrophenol, etc ., and carboxylic acids with low molecular weight.

HPLC和GC-MS结果表明,ClNBs主要被转化为氯酚、硝基酚、氯代硝基酚、硝基苯、氯苯和低分子的羧酸等物质。

The results show that: 27 compounds were identified at 600℃, and most of them were alkenes, alkanes, acids, alcohols and phenolic substances; geraniol was identified, and its relative content was 3.6, which shows that geranyl 8-methoxycoumarin-3-carboxylic acid ester can release a certain amount of geraniol at smoke temperature; geranyl 8-methoxycoumarin-3-carboxylic acid ester can improve and modify the flavor, enhance the notes of sweet aroma and bean aroma, and reduce the biting taste of cigarette smoke.

结果表明,600℃时,8-甲氧基-香豆素-3-甲酸香叶酯的热解产物中共鉴定出27种成分,主要为烯类、烷类、酸类、醇类、酚类;鉴定出香叶醇,且相对峰面积3.6,说明8-甲氧基-香豆素-3-甲酸香叶酯能在卷烟燃吸温度下释放出一定量的香叶醇;8-甲氧基-香豆素-3-甲酸香叶酯具有改善和修饰卷烟香气,增加甜韵和豆香香韵,减轻刺激性的作用。

The molecular charge distribution of the reactivator is affect the reactivating efficacy directly. Moreover its association with hydroximic acid dissociation constant pAa closely, and it will have a great impact on reactivating ability indirectly.(3) There is likely to exist front molecular interaction between Cholinesterase Reactivators and OPC-inhibited AChE, the action sites mainly lie on the aromatic ring, the substitute R and the hydroixic acid group. They act on the aromatic residues of AChE by Π-Π conjugation .(4) The reached results by Comparative Molecular Field Analysis is useful to design new higher efficacy derivatives for 1, 2, 4-oxadiazole class nonquaternary Cholinesterase Reactivators.

2复能剂分子的电荷分布直接影响复活活性,同时对肟酸解离常数pKa具有重要影响,间接影响复活能力;(3)复能剂与磷酰化酶可能存在前线轨道作用,作用部位可能主要在芳香环及其取代基R和肟基上,与AchE的芳香族残基发生л-л电子作用;(4)通过比较分子力场法研究可以指导1,2,4-oxadiazole类非季铵肟胆碱酯酶重活化剂新化合物的合成,可能得到活性更高的复能剂。

The performance and mechanism of corrosion inhibitions of POCA were studied bymethods such as weight-loss, electrochemistry, EDS, XPS and quantum chemistry. It isfound that POCA is cathodic corrosion inhibitor, having synergistic effect with HEDP andZn~(2+). The P and O atoms of phosphono have important electron density contribution toHOMO orbital and the electron gross orbital population is bigger than 1, so it is easy toform absorbing location between phosphono and metal resulting in good corrosioninhibition on mild steel.

通过利用失重法、电化学方法、扫描电镜、X光电子能谱、X-射线能谱和量子化学方法研究膦酰基羧酸的缓蚀性能及其机理,发现POCA是一种阴极型缓蚀剂,与HEDP、Zn~(2+)具有优良的协同增效作用;POCA分子中的膦酰基基团的P原子和O原子对HOMO轨道电荷密度贡献较大,且其轨道电子布居数均大于1,因此比较容易通过膦基与金属形成吸附位而对碳钢具有良好的缓蚀作用;对铜合金具有一定的腐蚀作用,但腐蚀作用比HEDP等有机膦药剂要小得多,同时与BTA具有优良的相容性,添加1mg/L的BTA则可以有效地防止铜合金的腐蚀。

The article is summarized as follows to its namely. 1 manage changes property Tekturna piece in advocate composition A Li Kelun exists with the form of acerbity salt of half rich horse, chemical name is (2S, 4S, 5S, acyl of 7S)-N-(2- amino armour base - 2- methylic propyl)- 5- amino - 4- hydroxyl - 2, 2 different of 7- propyl - 8-4- armour oxygen - 3-3- armour...

本文即对其概述如下。1理化性质Tekturna片中主成分阿利克仑以半富马酸盐的形式存在,化学名为(2S,4S,5S,7S)-N-(2-氨基甲酰基-2-甲基丙基)-5-氨基-4-羟基-2,7-二异丙基-8-4-甲氧-3-3-甲。。。

The Scandia doped tungsten powders were made by both liquid-solid doping method and liquid-liquid doping method on the basis of previous researches. The study shows that on the basis of improving pressing and sintering process, we can obtain sub-micron porous bodies with proper porosities.

研究表明在改进压制、烧结技术的基础上,可以获得具有适当孔度的亚微米结构多孔基体,氧化钪在基体中的分布得到进一步改善,在这种基体中铝酸盐的浸渍率可以达到常规浸渍阴极的要求。

Methods Porcine bile duct and ureter were treated using detergent sodium dodecylsulphate and 1% Triton X-100 to prepare the acellular lumens matrix. The toxic effects of different concentrations of acellular lumens matrix extract were tested by MTT to assess the proliferation of human scarfskin fibroblasts. The cytotoxicity of the target biomaterial was graded according to the national standards. The growth manner of the human intrahepatic bile duct endothelial cells seeded on the acellular lumens matrix was studied after 20 d under scanning electron microscopy.

采用十二烷基磺酸钠、Triton X-100处理封闭群小香猪输尿管和胆管,获得去细胞管腔基质支架材料; MTT法检测基质支架材料的不同浓度浸提液对细胞增殖的影响,并按医用生物材料细胞毒性分级标准进行评级;在基质支架材料上种植人肝内胆管上皮细胞,于接种后20 d通过扫描电镜观察人肝内胆管上皮细胞在支架上的生长情况。

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