羧基化

The present invention relates to a process for rapid solution synthesis of a peptide, the process comprising repetitive cycles of steps-: a coupling step, using an excess of an activated carboxylic component to acylate an amino component, a quenching step in which a scavenger is used to remove residual activated carboxylic functions, wherein the scavenger may also be used for deprotection of the growing peptide, one or more aqueous extractions and optionally, a separate deprotection step, followed by one or more aqueous extractions, characterised in that the process comprises at least one step, referred to as step, in which an amine or a thiol comprising a free anion or a latent anion is used as a scavenger of residual activated carboxylic functions.

本发明涉及快速溶液合成肽的方法，该方法包括步骤-的重复循环：偶联步骤，使用过量的活化羧基成分酰化氨基成分，淬灭步骤，在该步骤中使用清除剂除去残余的活化羧基官能团，其中该清除剂还可以用于使生长中的肽去保护，一或多个水抽提和任选地，独立的去保护步骤，之后进行一或多次水抽提，其特征在于该方法包括至少一个步骤，称作步骤，在该步骤中包含自由阴离子或潜阴离子的胺或硫醇用作残余活化羧基官能团的清除剂。

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 some cases, its epimer 4 was also obtained. 22 compounds were synthesized, among them 18 were new.3. Using the intramolecular Pictet-Spengler reaction to form the pentacyclic skeleton of Et-743, the byproducts 25 were obtained under various conditions. The structures of them were determined to be 1, 2-dihydro-isoquinoline compounds, and the mechanism of the reaction was proposed.B. The synthesis of the analogs of Et-743Because of the failure of removing the protective groups in compounds 14, the synthetic strategy was adjusted.

对于苄基保护的羟基化合物13a，顺利得到化合物30，然后与不同的羧酸反应得到18个酯化合物33-50；对于苄氧羰基保护的氨基化合物13b，由于脱除保护基的化合物31在空气中不稳定，所以我们采取不经分离纯化，直接与羧酸反应得到酰胺化合物53-62，然后再分别对其C-21位的羰基进行还原氰基化，得到10个酰胺目标化合物63-72，另外，我们还对羟基转化为氨基的反应进行了探索。3。

The new compound,2- oxo-propionic acid p-carboxylphenyl hydrazone,was synthesized by the condensation reaction of 2- oxo-propionic acid and p-carboxylphenyl hydrazine which was prepared from p-aminobenzoic acid by diazotization and reduction.

以对氨基苯甲酸为原料，经过重氮化反应和还原反应，合成了对羧基苯肼(2)；2与2-羰基丙酸缩合得到新化合物2-羰基丙酸缩对羧基苯腙，其结构经UV，荧光光谱，1H NMR，13C NMR，IR和元素分析表征。

Therefore esterification crosslinked reactionbetween polyearboxylic acid and wood can be quantitatively determined.According toexperiment results of stereoscopic configuration choices by crosslinking agents,crosslinkingreaction between model of reaction intermediate and wood,and the intermediate characteristic incrosslinking reaction,crosslinking reaction intermediate was proofed.We can infercrosslinking reactions between polycarboxylicacid and wood want through a mechanism of twosteps reaction process,the first cyclic anhydrides were formed as intermediates by dehydratingbetween hydroxyls in polycarboxylic acids,second esters were occurred by substitution reactionbetween wood hydroxyls and cyclic anhydrides.

从而可全面定量表征木材与多元羧酸类化合物的酯化交联反应；依据交联剂立体构型选择性、反应中间体模型物与木材的交联反应和交联反应中间体的波谱特征实验结果，证实了交联反应中间体，因此可以推测：多元羧酸类化合物与木材化学组分的交联反应是经历两步反应的机理，首先多元羧酸中相邻羧基的羟基之间脱水形成五元环酸酐中间体，然后木材的羟基与酸酐发生亲核取代反应形成酯。

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。

Spiral Spirobifluorene acetylated is oxidated by m-chloroperoxybenzoic acid and hydrolyzed by sodium hydroxide ,obtaining 2,2 '- dihydroxy -9,9'- spiral Spirobifluorene .Through nitrification,Reduced by hydrazine hydrate, we may get the 2,2 '- diamino -9,9'- spiral Spirobifluorene which are characterizated by IR, 1H-NMR !

L-酒石酸和乙醇酯化得到酒石酸二乙酯，将保护羧基保护起来，然后用碘甲烷在2，3-位上两个甲基，得到2，3-二甲氧基-酒石酸二乙酯，再用氢氧化钠将其水解，得到2，3-二甲氧基-酒石酸，用五氯化磷将羧基酰化，得到2，3-二甲氧基- 1，4-丁二酰氯，经过与二环己胺反应，得到拆分配体2，3-二甲氧基–N，N，N'，N'-四环己丁二酰胺。

Mol/L. 3 A study on the ECL of acridinum esters including 10--acridinium-9-carboxyl-phenyl-ester iodinate and 10-methyl-9-(p-formylphenyl)-acrdiniumfluorosulphonate in neutral solution was carried out. It was found both CACPEI and MFPA give strong ECL in KNO〓 solution when an appropriate voltage was applied on Pt electrode.

本文研究了碘化10-乙羧基吖啶-9-羧酸苯酯和对甲酰基苯基-10-甲基吖啶-9-羧酸酯氟磺酸盐的ECL行为，发现在中性KNO〓介质中，这两种吖啶酯都能在一定的电位下产生很强的ECL信号，考察了各种影响因素，确定了发光的最佳条件，探讨了可能的发光机理。

The improved method of konjac glucomannan carboxy methylation was proposed in this paper according to the effects of deacetylation. Carboxymethyl KGM were synthesized by blending KGM with etherification agent first and then basifying and catalyzing in ethanol. Basifying first and then etherifying prepared traditional carboxymethyl KGM.

针对脱乙酰基的这种影响进行羧甲基化方法的改进，在乙醇介质中先混合醚化剂，再进行碱化催化反应制备羧甲基魔芋葡甘聚糖，并通过与传统的先碱化再醚化的KGM羧甲基改性方法比较，达到乙酰基脱出顺序上的不同。

We have synthesized 4,4'-dinitro-3 4''-dimethyl triphenylamine,(1), in 84% yield in an one-step condensation process between 3,4-dimethyl aniline and 4-fluoro-nitrobenzene. After the auto-oxidation of (1) and the subsequent hydrogenation of the nitro-groups, an AB2 type triphenylamine polyimide intermediate bearing two amine groups and one acid-anhydride group each on individual phenyl ring,{AB2 PI Intermediate}, was prepared successfully. The yields of the autoxidation and the hydrogenation steps are 81% and 90% respectively.

中文摘要本研究以3，4-二甲苯胺及4-氟硝基苯为原料，经一步骤缩合反应得到产率为84 %之4，4'-二硝基-3&，4&-二甲基三苯胺(1)，由(1)经自氧化法后再以氢化法还原硝基，成功地制备出带有二胺基与一羧基的三官能基之AB2型三苯胺中间体(AB2型PI中间体)，自氧化反应与氢化法的产率各为81%及90%。

Do you know, i need you to come back

你知道吗，我需要你回来

Yang yinshu、Wang xiangsheng、Li decang,The first discovery of haemaphysalis conicinna.

1〕 杨银书，王祥生，李德昌。安徽省首次发现嗜群血蜱。