内酯化

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。

Objective To study the stability of ligustilide and the inclusion process in β-cyclodextrin to avoid its isomerization.

目的 考察藁本内酯的稳定性，并采用β-环糊精包合，避免藁本内酯的异构化。

During these years (1997-2000) in the research area of annonaceous acetogenins 5 natural products and a number of chiral-pure analogs of annonaceous acetogenins have been synthesized using sugars as the starting materials. Their high activity and selectivity against cell line of colon tumor and a relationship between activity and configuration have been found too. In the respect of inhibitor of sialidase two new methodologies for the synthesis of chiral-pure 3-deoxy-ulosonic acid using hetero-Diels-Alder reaction or asymmetric propargylation as the key reaction were developed. On the topic of anti-leukemia marine natural product clavulactone a synthetic method based on the free radical cyclization and starting from sugar has been developed. In other title of PKC inhibited agent sphingosine a new synthetic route with SN2' as the key reaction has also been disclosed.

项目期间（1997-2000）在番荔枝内酯方面从糖出发合成了五个天然产物和一批手性纯的类似物，它们对肠癌细胞有很高的活性和选择性，并与构型有关；在唾液酸酶抑制剂方面发展了二类全新手性纯高碳糖的合成方法－杂原子D－A反应或丙炔基不对称加成为关键的反应；抗白血病海洋天然产物群柱虫内酯方面研究了由糖出发和自由基环化反应的合成方法；对PKC 起抑制作用的鞘氨醇方面也开创了新的合成途径－由糖出发并以SN2'反应为关键反应。

The catalysts such as tetraphenyl tin,aluminium isopropoxide and boron trifluoride etherate complex were used to catalyze the copolymerization.In addition,the copolyester can be given by copolycondensation after monomers were hydrolyzed by phosphoric acid.Boron trifluoride etherate complex was chosen as the catalyst because the catalytic activity was the best among the catalysts.

由于γ-戊内酯为五元环结构，难以进行开环聚合，因此分别考察了四苯基锡、异丙醇铝、三氟化硼乙醚络合物等催化剂，以及以磷酸为催化剂的水解缩聚反应，结果发现三氟化硼乙醚络合物的催化活性最高，因此选择三氟化硼乙醚为本体开环聚合的催化剂。

Compared with the previous method, the improved route can provide directly a spheroid form of immobilized lipase particles of which the size can be controlled by adding non-ionic surfactants during the preparation process so as to increase the recovery rate of enzyme as well as decrease the external diffusional restriction which can diminish the enzyme activity. The improved method can also alter the hydrophobicity and microstructure of the immobilized enzyme matrix by changing the molar ratios of different alkoxyl silanes so as to enhance the enzyme activity by a"surface active effect"and eliminating the internal diffusional restriction.

与前人的制备方法相比，改进的方法可直接制得球形的固定化酶颗粒，而且颗粒的大小可以通过在制备过程中加入非离子型表面活性剂加以控制，从而可以提高固定化过程的酶活回收率和减小外扩散效应对酶的表观催化活力的影响；改进的方法还可以通过改变原料硅氧烷的种类及配比来改变最终制得的固定化载体的疏水性质及微观结构，从而通过对脂肪酶的&界面活化&作用和减小内扩散效应提高固定化脂肪酶的表观酯化活力。

One synthetic strategy started fromγ-butyrolactone 38, from which a cyclohexadiene intermediate 30 was prepared in an overall yield of 44% in a 7-step procedure after y-butyrolactone underwent a-bromination, dehydrobromination, Diels-Alder reaction, aminolysis, benzylation, bromination and dehydrobromination, with the key step being the Diels-Alder reaction under harsh condition.

其中一个路线从γ-丁内酯38开始，连续经过α-溴化、脱溴化氢、Diels-Alder反应、胺解、苄基化、溴化和脱溴化氢共7步反应，制备了一个环己二烯衍生物30，总产率44％，关键步骤是高温高压下Diels-Alder反应。

Mission:"equality and mutual benefit, reputation first, unity and cooperation and friendship between the long-term" supply products: ethylenediamine; diethylamide; triethylamine; Diethylenetriamine; three ethylene diamine; three ethylene amines 40; 40 Five ethylene amines; five ethylene amines 6; caprolactam; DMF; allyl amine; N, N dimethylaniline; propylamine; are butylamine; are TOA; 3 Poly Cyanamide; 1,2 c diamine; ethanolamine; diethanolamine, triethanolamine; potassium iodide, potassium hydroxide, potassium permanganate, toluene, xylene, toluene of chlorine ; Acetone, butanone; acetylacetone; ethyl acetate, butyl acetate; Y-butyrolactone; DMC; acetyl of methyl acetate; Sanfu acetyl acid; Sanfu acetyl B Ethyl; methanol, ethanol, isopropanol; propylene glycol; glycerol; propargyl alcohol; 1.3 propylene glycol; xylitol; acetic acid; have acid; mercaptoacetic acid; vary Bitterness; adipic acid; trifluoroacetic acid; oxalic acid, the amino acid; o-amygdalin acid; DL-Acid; anhydrous piperazine; six non-piperazine, furfural, castor oil, ethylene Aldehyde; glutaraldehyde, multi-POM; isopropyl ether; anisole; tetrahydropyrrole; pure pyridine; 1.2 dichloroethane; methylene chloride, chloroform, carbon tetrachloride; hydrazine hydrate; Nonylphenol;-m-cresol; Se phenol; phenol; the tert-butyl phenol; Titanium Dioxide; iron; full Tangfen; Bisphenol A; azo two different nitrile; sodium azide; sodium carbonate ; Sodium chloride; iron oxide; cuprous chloride; thionyl chloride; D4; sodium bicarbonate; ammonia, potassium chloride; anhydrous sodium sulphite; ammonium persulfate; glycol Dingmi; B Glycol ether; calcium chloride; cyclohexanone; cyclohexane, methyl tertiary butyl ether, potassium carbonate, ferric chloride, potassium nitrate; Linsuansanna; zinc oxide; sodium nitrite; antimony oxide; Tartrate; OP-10; TX-10; tablets base; AES; sodium benzoate, sodium citrate; partial sodium silicate, sodium perborate, a sodium carbonate, sodium benzene; Asia sodium chlorate; Wuluo Care products; urea; hydrochloric acid, sulfuric acid, lactic acid; amino acid, hydrogen peroxide, ammonium bicarbonate

公司宗旨：&平等互利，信誉至上，团结合作，友谊长久&乙二胺；二乙胺；三乙胺；二乙烯三胺；三乙烯二胺；三乙烯四胺；四乙烯五胺；五乙烯六胺；己内酰胺；二甲基甲酰胺；烯丙基胺；N，N二甲基苯胺；正丙胺；正丁胺；正辛胺；三聚氰胺；1，2丙二胺；一乙醇胺；二乙醇胺；三乙醇胺；碘化钾；氢氧化钾；高锰酸钾；甲苯；二甲苯；对氯甲苯；丙酮；丁酮；乙酰丙酮；醋酸乙酯；醋酸丁酯；Y-丁内酯；碳酸二甲酯；乙酰乙酸甲酯；三伏乙酰乙酸；三伏乙酰乙酸乙酯；甲醇；无水乙醇；异丙醇；丙二醇；丙三醇；丙炔醇；1.3丙二醇；木糖醇；冰醋酸；己醛酸；巯基乙酸；异辛酸；己二酸；三氟乙酸；乙二酸；对氨基苯乙酸；邻氯苦杏仁酸；DL-扁桃酸；无水哌嗪；六无哌嗪；糠醛；蓖麻油；乙二醛；戊二醛；多聚甲醛；异丙醚；苯甲醚；四氢吡咯；纯吡啶；1.2二氯乙烷；二氯甲烷；三氯甲烷；四氯化碳；水合肼；壬基酚；纯间甲酚；硒酚；苯酚；对叔丁基苯酚；钛白粉；铁粉；全糖粉；双酚A；偶氮二异丁腈；叠氮化钠；碳酸钠；氯化钠；三氧化二铁；氯化亚铜；氯化亚砜；D4；碳酸氢钠；氨水；氯化钾；无水亚硫酸钠；过硫酸铵；乙二醇丁醚；乙二醇乙醚；氯化钙；环己酮；环己烷；甲基叔丁基醚；碳酸钾；三氯化铁；硝酸钾；磷酸三钠；氧化锌；亚硝酸钠；氧化锑；酒石酸；OP-10；TX-10；粒碱；AES；苯甲酸钠；柠檬酸钠；偏硅酸钠；过硼酸钠；过碳酸钠；苯磺酸钠；亚氯酸钠；乌洛托品；尿素；盐酸；硫酸；乳酸；氨基磺酸；双氧水；碳酸氢铵

The dissertation mainly consists of two parts:1. The Reaction Chemistry of Alkynes under Palladium Catalysis Part 1 studies the reaction α,β-unsaturated carbonyl compounds with alkenylpalladium intermediate generated by nucleopalladation, and discovered 1 the Pd-catalyzed tandem addition reaction of halides, alkynes and α,β-unsaturated carbonyls,2 the four-component tandem addition reaction of halides, alkynes and α,β-unsaturated carbonyls, 3 the tandem intramolecular oxypalladation-conjugate additionreaction of alkynoic acids with α,β-enals. These new reactions provide notonly efficient highly stereoselective methods for the synthesis of γ,δ-unsaturated,polyunsaturated carbonyl compounds and γ-lactonic aldehydes, but also thebasic transformations for a number of C-C bond formation reactions which can be usedto design synthesis of many acyclic, cyclic or polycyclic compounds.

本论文的主要工作分为两个部分：一、钯催化下炔烃的反应化学在本小组前人工作的基础上，我们详细研究了炔烃亲核钯化产生的烯基钯中间体与α，β-不饱和羰基化合物的反应，发现两价钯催化下卤离子-炔烃-α，β-不饱和醛酮的串联加成反应、卤离子-炔烃-α，β-不饱和醛酮的西组分串联加成及炔酸分子内氧钯化-串联Michael型加成反应；由此发展了γ，δ-不饱和醛酮、多不饱和羰基化合物和带有醛酮基侧链的γ-丁内酯衍生物的高立体选择性合成方法，这一过量卤离子存在下的烯基钯对α，β-不饱和羰基化合物共轭加成反应的发现，为大量碳-碳键形成反应的实现提供了基础，使我们能够从这一基本反应出发，设计和开发多种分子内、分子间的碳碳成键反应，以好的立体、区域选择性组建开链、环状及多环类型的化合物。

Objective:To study the effect of spironolactone inhibiting proliferation on cultured myocardiac myofibroblasts and explore its possible mechanisms.

目的：研究螺内酯对培养的心肌成纤维细胞增殖的作用，揭示螺内酯抑制心肌纤维化的可能机制。

Cellulose acetate butyrate,which is widely applied as coatings additive, is synthesized in the heterogeneous system. The activation is required because of the strong hydrogen intramolecular and intermolecular bondings and the regulation of the crystalline region in cellulose microfibrils.

中文摘要纤维素醋酸丁酸酯（Cellulose acetate butyrate是一种广泛应用于涂料工业的添加剂，由于纤维素具有分子内与分子间强氢键作用以及纤维素纤维的局部规整的结晶序列等特征，一般纤维素在酯化反应前都需要进行预活化处理，工业上纤维素醋酸丁酸酯的合成方法一般都在非均相体系中进行的。

She gently rebuff ed him, but agreed that they could be friends

她婉言拒绝了，但同意作为朋友相处。

If in the penal farm, you were sure to be criticized.

要是在劳改农场，你等着挨绳子吧！