酰化作用

We investigated constituent of triterpenoid saponins ofAlbizzia, two new compounds together with two known compounds were isolated from Albizzia julibrissin Durazz. by using column chromatography (macroreticular resin, silica gel, Sephadex gel, reverse phase silica gel),preparative HPLC methods et al.On the basis of spectroscopic analysis, including IR,ESI-MS,~1H-NMR,~(13)C-NMR,HMBC,HMQC,~1H-~1HCOSY and chemical methods, the structure of two new compounds were identified as 3 - O -[β-D-xylopyranosyl(1→2)-β-D-fucopyranosyl (1→6)-β- D -2- deoxy - 2 - acetoamidoglucopyranosyl] -21-O-[(6S)-2- trans- 2,6-dimethyl - 6 - O-β- D - quinovopyranosyl -2,7- octadienoyl] - acacic acid- 28 - O-β-D-glucopyranosyl(1→3)[α-L-arabinofuranosyl(1→4)]-α-L-rhamnopyranosyl(1→2)-β-D-glucopyranoside acacic acid 3- O -β- D- glucopyranosy(1→3)-β- D- fucopyranosl(1→6) [β-D- xylopyranosyl (1→2)]-β-D-glucopyranoside ;two known compounds were acacic acid lactone 3- O -β-D- xylopyranosyl-(1→2)-β-D-fucopyranosl (1→6)- 2-deoxy -2 -acetoamido -β-D- glucopyranoside ; acacic acid lactone 3- O-β-D-xylopyranosyl(1→2)-α-L- arabinopyranosl (1→6)- 2- deoxy - 2- acetoamido -β-D-glucopyranoside . The study lays chemical foundation and chemical reference substance for enhancing quality standard of Albizzia julibrissin Durazz.

本研究论文在综述国内外对合欢属Albizzia三萜皂苷化学成分和药理作用研究进展的基础上，利用传统植化分离手段和现代分离技术，包括大孔树脂、硅胶、葡聚糖凝胶、反相硅胶等柱色谱，制备高效液相色谱法等技术从中药合欢皮中分离得到了4个化合物，其中，2个新化合物和2个己知化合物，并进一步通过现代分析技术IR，ESI-MS，~1H-NMR，~(13C-NMR，HMBC，HMQC，~1H-~1HCOSY等和化学方法鉴定了2个新化合物的结构分别是：3-O-[β-D-吡喃木糖基(1→2)-β-D-吡喃夫糖基(1→6)-β-D-2-去氧-2-乙酰氨基吡喃葡萄糖基]-21-O-[(6S)-2-反式-2，6-二甲基-6-O-β-D-吡喃鸡纳糖基-2，7-辛二烯酸基]-金合欢酸-28-O-α-L-呋喃阿拉伯糖基(1→4)[β-D-吡喃葡萄糖基(1→3)]-α-L-吡喃鼠李糖基(1→2)-β-D-吡喃葡萄糖苷，金合欢酸3-O-β-D-吡喃葡萄糖基(1→3)-β-D-吡喃夫糖基(1→6)[β-D-吡喃木糖基(1→2)]-β-D-吡喃葡萄糖苷；2个已知化合物结构分别是：金和欢酸内酯3-O-β-D-吡喃木糖基(1→2)-β-D-吡喃夫糖基(1→6)-β-D-2-去氧-2-乙酰氨基吡喃葡萄糖苷，金和欢酸内酯3-O-β-D-吡喃木糖基(1→2)-α-L-吡喃阿拉伯糖基(1→6)-β-D-2-去氧-2-乙酰氨基吡喃葡萄糖苷。

The better reaction conditions are as follows: Reaction temperature is 40°C, Reaction time is 5 hour; the ratio of L - phenylalanine to acetic acid and N - formyl - L- aspartyl anhydrideis 1:10.2:1.1, Its yield is 95.4%.

在查阅文献的基础上，得到较优的α-L-天冬氨酰L-苯丙氨酸甲脂盐酸盐的合成方案，在甲醇一水体系中，N-甲酰-α-L-天冬氨酰-L-苯丙氨酸在浓盐酸的作用下60℃水解90分钟，后冷却到15℃加入浓盐酸在20～30℃保温反应96小时，进行甲脂化，形成甲脂盐酸盐，结晶析出。

PartⅡ: N-phosphoryl amino acids have many biomimic reactions and the co-participation of the three functional group of phosphoryl, carboxyl and theamino acids side chain are essential for these reactions to occur. To study themechanism and the intrinsic relationship of these three groups will enlight thestudy on the mechanism of enzymatic reaction, the origin of life and otherproblems in the life science.

第二部分：N-磷酰氨基酸的多种仿生化反应是磷酰基、羧基、和侧链基团协同作用的结果，对其反应机理的研究，将对生化反应和生命起源中磷的作用有着重要的意义。

In part one, the reactions of some active fluorine-containing compounds such as 2, 2-dihydropolyfluoroalkanoic acids and ethyl 2-hydropolyfluoroalkenoates were studied and various fluorine-containing heterocyclic compounds were synthesized. Using 2, 2-dihydropolyfluoroalkanoic acids as the starting material, 4-fluoroalkyl quinolin-2-ols, 2- [ -1-hydropolyfluoro-1-alkenyl] -4H-3, 1-benzoxazin-4-ones, 1-aryl -4, 9-dihydro-3-fluoro-alkyl-1H-pyrazo [3, 4-b] quinolin-4-ones, 5-fluoroalkyl-12H-quin olino [2, 1-b] quinazolin-12-ones, 4-fluoroalkyl-1, 3-dihydro-1, 5-benzodiazepin-2-ones and 4-fluoroalkyl-2H-pyrido [1, 2-a] pyrimidin-2-ones were synthesized through its condensation reaction with anilines, anthranilic acid, N'-aryl-o-aminobenzamides, o-nitro aniline, o-amino pyridine and their derivatives and the subsequent transformations. 5-Fluoroalkyl isoxazolidines, 3-fluoro-3-fluoroalkylisoxazolidino [4, 3-c] quinolin-4-ones, 3-fluoroalkylisoxazolino [4, 3-c] quinolin-4-ones and 2-aryl-3per fluoroacylindoles were synthesized by inter-and intramolecular 1, 3-dipolar cycloaddition of fluorine-containing olefins and nitrones.

第二部分，我们研究了α，α-二氟苄基卤类化合物的亚磺化脱卤反应、产物的转化及全氟烷基亚磺酸盐与芳环化合物的全氟烷基化反应，发现全氟苄基碘或溴及α，α一二氟苄基溴在保险粉等亚磺化脱卤试剂引发下可生成相应的亚磺酸盐；全氟苄基亚磺酸盐与氯气或溴反应可生成全氟苄基磺酰氯或磺酰溴；在烯烃存在下，全氟苄基碘则与烯烃发生加成反应，生成相应的1：1加成产物；在三价醋酸锰的作用下，部分芳香化合物如茴香醚，二甲氧基苯，吡啶，喹啉等可以和过量的全氟烷基亚磺酸盐发生双全氟烷基化反应，反应表现出一定的区域选择性，产率良好。

Methods: A model to evaluate lymphocyte proliferation stimulated with a polyclonal activator, concanavalin A, was established by vital dye carboxyl fluorescin diacetate succinmidyl ester labeling technique. Effects of the different doses of anisomycin on the lymphocyte proliferation were estimated by flow cytometry and MTT methods. The propidium iodide labeling technique was applied to assay the effect of the different doses of anisomycin on changes of the lymphocyte cell-cycle stimulated by ConA or by phorbol ester plus Ionomycin. The percentage of the expression level of CD69 and CD25 on the activated lymphocytes was evaluated by fluorescin-conjugated monoclonal antibody double labeling technique.

以活体染料羧基荧光素乙酰乙酸琥珀酰亚胺酯染色，建立在多克隆刺激剂刀豆蛋白A刺激下评价小鼠淋巴细胞增殖的模型，通过流式细胞术和MTT法分析茴香霉素在不同剂量下对淋巴细胞增殖的作用；采用碘化丙锭染色分析茴香霉素对ConA或佛波醇酯加离子霉素刺激的小鼠淋巴细胞周期变化的作用；利用荧光标记的单克隆抗体双染技术和流式细胞术观察茴香霉素对小鼠CD3~+T细胞早期及中期活化标志分子CD69和CD25表达的影响。

(1)PAL is better entrapped by PAG with a T∶C ratio of 8∶30.(2)PAL immobilized by glutaric dialdehyde on Bio-Gel P-300 is better than by CDC.(3)The best one is the dehydration and redehydration method.(4)Immobilized and permeated PAL active yeast cells are resistant to trypsin digestion and retain its PAL activity.

(1)固定化酶活性采用T∶C比为8∶30明显高于8∶19；(2)以戊二醛将PAL固定于Bio-GelP300优于用DCD固定化的酶；(3)质脂体包被中以脱水再加水法对酶活性影响较少，脂类组成以磷脂酰胆碱：胆固醇：磷脂酰丝氨酸比值7∶2∶1最好；(4)固定化PAL活性酵母细胞能较好地抵抗人工肠液中胰蛋白酶的水解作用，亦能明显降低苯丙氨酸的浓度。

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%。

In acid pulp, the depressing abilities of reagents on diaspore are in the order of hydroxamic acid starch＞dialdehyde starch＞carboxymethyl starch＞cationic starch＞primary starch. In addition, hydroxamic acid starch and carboxymethyl starch can activate kaolinite without influence on the recoveries of pyrophyllite and illite, so the two reagents have great potential and prospect to be the depressant of diaspore and the activator of kaolinite in bauxite reverse flotation.(3) By oximation of the copolymer of acrylamide and methyl acrylate, hydroxamic acid polyacrylamide is synthesized.

3对丙烯酰胺和丙烯酸甲酯的共聚物肟化制得氧肟酸聚丙烯酰胺，将它同非离子聚丙烯酰胺、阴离子聚丙烯酰胺、阳离子聚丙烯酰胺和两性聚丙烯酰胺分别应用于四种矿物的单矿物浮选试验，结果显示，改性聚丙烯酰胺对一水硬铝石、高岭石和伊利石均具有活化作用，其中，药剂对高岭石的活化最强，使它的回收率在整个pH值范围达到80％左右，在一定pH条件下超过一水硬铝石的回收率，解决了高岭石难浮选的问题。

The famciclovir was synthesized from purine by a series of steps by Acylation, Decarboxylation, Reduction ,and so on; Derivatives of these intermediates is described from the 6-chloro- 9H- purin-2-amine as raw materials in different conditions when the iodine and bromide were synthesized with the addition of two intermediate 6-bromo-9H-purin-2-amine and 6-iodo-9H-purin-2-amine; There is elaborated from the main part of a acetophenone, urineaminohydrochloride, phenylhydrazine, ethyl acetoacetate as raw material through a series of reactions to synthetic 3-phenyl-4-formylphenyl pyrazole and 5-chloro-3-methyl-1-phenyl-1H-pyrazole-4-aldehyde two pyrazole aldehyde, and then with 2-amino-6-chlorine-9-(2-methicillin-oxo-co-methyl-4-yl) purine reaction of the two new pyrazole purine Schiff bases.

本论文主是采用以鸟嘌呤为原料，经过一系列的酰基化，脱羧，还原等反应作用下最终得到了产物2-氨基-9-(4-乙酰氧基-3-乙酰氧基甲基丁基)嘌呤；其中的中间体衍生物主要是阐述从以2-氨基-6-氯鸟嘌呤为原料通过在不同的条件下进行溴代与碘代分别合成了另外两种中间体2-氨基-6-溴鸟嘌呤及2-氨基-6-碘鸟嘌呤；还有一部分主要是阐述从以苯乙酮，盐酸氨基脲，苯肼，乙酰乙酸乙酯为原料通过一系列的反应先合成3-苯基-4-醛基吡唑及5-氯-3-甲基-1-苯基-1H-吡唑-4-甲醛这两个吡唑醛，然后再与2-氨基-6-氯-9-(2-甲氧羰基丁酸甲酯-4-基)嘌呤反应得到了两个新型的吡唑嘌呤席夫碱

We reported the effect of several kinds of surfactants on the fluorescent properties of a new watersoluble fluorescent polymer (PPESO3) synthesized in this paper.

研究几种不同类型的表面活性剂对所合成的新型水溶性荧光聚合物PPESO3聚[5，3-二(3-磺酰化丙氧基-1，4-苯撑乙烯]的作用。

We have no common name for a mime of Sophron or Xenarchus and a Socratic Conversation; and we should still be without one even if the imitation in the two instances were in trimeters or elegiacs or some other kind of verse--though it is the way with people to tack on 'poet' to the name of a metre, and talk of elegiac-poets and epic-poets, thinking that they call them poets not by reason of the imitative nature of their work, but indiscriminately by reason of the metre they write in.

索夫农 、森那库斯和苏格拉底式的对话采用的模仿没有一个公共的名称；三音步诗、挽歌体或其他类型的诗的模仿也没有——人们把&诗人&这一名词和格律名称结合到一起，称之为挽歌体诗人或者史诗诗人，他们被称为诗人，似乎只是因为遵守格律写作，而非他们作品的模仿本质。

The relationship between communicative competence and grammar teaching should be that of the ends and the means.

交际能力和语法的关系应该是目标与途径的关系。