化学合成

Methods To adopt the intube method of Strawb,different concentration and dosage of garlicin were applied to irritate and flow.

大蒜素为大蒜提取物，已能化学方法人工合成应用。

Several anti-tumor cell lines and carbonic anhydrase Ⅱ model were established. More than 10000 compounds and extracts from plants were screened using these models and about 10 compounds showed strong inhibitory activities. Two species of plants Inula helianthus-aquatica and Saussurea deltoidea were chosen to investigate chemical and bioactivity constituents based on the results of screening of extracts and fractions. 58 compounds were isolated and identified from these two plants, 6 compounds were found to be new and 14 compounds showed anti-tumor activities. We also studied the anti-tumor mechanism of the compound bigelovin isolated from Inula helianthus-aquatica. Bigelovin was found with apoptotic activity against cell line U266 by lowering the amount of important transcription factor E2F-1 which inhibits the cell cycle at G0/G1 stage. Docking study on 7 natural new phenolic inhibitors of CA Ⅱ and 3D-QSAR study on 61 sulfonamide inhibitors of CA Ⅱwere also investigated. The calculated results were in good correlation with experimental results.

基于以上两种重要疾病和研究组方向，本论文工作开展了多个肿瘤细胞株和碳酸酐酶Ⅱ靶标模型的建立和筛选工作，累计筛选1万多个/次样品，发现10余个活性较强化合物；从粗提取物筛选结果中选取两种抗肿瘤活性强的菊科植物水朝阳旋覆花(Inula helianthus-aquatica)和三角叶凤毛菊进行了系统化学和活性成分研究，分离鉴定了58个化合物，发现6个新化合物和14个抗肿瘤活性化合物；通过合作对水朝阳旋覆花中活性较强的bigelovin进行了抗肿瘤作用机制研究，发现它可能是通过降低G2期重要的转录因子E2F-1，致使细胞周期阻滞在G0/G1期，引起多发性骨髓瘤U266细胞凋亡；开展了7个新的天然酚类CAⅡ抑制剂的对接研究和61个合成的系列磺酰胺类CAⅡ抑制剂的3D-QSAR分析，结果表明计算与实验一致。

Chapter 6: Iodobenzene diacetate-mediated reactions of methylenecyclopropanes, vinylidenecyclopropanes and a methylenecyclobutane with phthalhydrazine give the corresponding [3+2] cycloaddition products in good yields under mild conditions. In these reactions, phthalhydrazine was transformed to a 1,3-dipole intermediate in the presence of iodobenzene diacetate. A plausible reaction mechanism has been proposed.

本论文对亚甲基环丙烷类化合物的一些化学反应性能进行了研究，发现了亚甲基环丙烷类化合物在不同试剂或不同催化剂作用下的一些新的化学转化并合成了一些结构简单但具有潜在应用价值的有机小分子。

The oxygen nonstoichiometry values of the materials were measured by iodometric titration method. The results indicate the oxygen nonstoichiometry of doped LaCoO3-δ ceramics increase with increasing Co/Fe ratio.

采用碘滴定法测定了合成氧化物的氧非化学计量值，结果说明氧空位浓度随掺杂铁含量的提高而降低。

The results indicate that polyborazine precursor prepared at 150℃ for 10 h and propylamine/isopropylamine molar ratio 2:1, could possess nearly linear molecule skeleton and he prone to melt spinnability. When melt at 90℃, the precursor fibers are prepared with average diameter 10-20μm and BC1.27 N1.52 H structure. After curing process and sintered in NH3 at 1200℃, the near-stoichiometric BN fibers was obtained, which proved this precursor is apt for preparation of BN fibers.

结果表明，当正丙胺／异丙胺摩尔比为2：1，聚合温度为150℃，反应时间为10h时，合成产物具有近似线性分子结构，熔点为90℃，具有良好的成丝性，可获得平均直径10~20μm，组成为BC1.27N1.52H的先驱体纤维，先驱体纤维再经不熔化处理及1200℃氨气高温锻烧等工艺可获得近化学计量比的氮化硼纤维。

The α-methylenecyclopentanone, as an isostere of α-methylene-γ-lactone, within the molecules of diterpenes may be as effective as α-methylene-γ-lactone towards various sulfhydry-containing enzymes.

然而，由于α-亚甲基-γ-丁内酯结构内在的化学活性太强，尽管这些合成的小分子化合物仍具有抗癌或抗炎活性，但并没有达到降低毒性，提高选择性的目的。

Fourteen new pyrethroids containing isoxazole were designed and synthesized from 4-isopropyl-3-substituted phenyl-5-hydroxyl isoxazoles as major material, whose structures were also characterized by IR, 1H NMR and elemental analysis.

以4-异丙基-3-取代苯基-5-羟基异噁唑和3-苯氧基苄基溴为原料，三乙胺为缚酸剂，设计并合成了14个未见报道的4-异丙基-3-取代苯基-5-异噁唑基-(3'-苯氧基)苄基醚。通过红外光谱、核磁共振、元素分析等手段，确证了它们的化学结构。

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。

Our group has prepared a series of ladderlike polysiloxane via"supramolecular template-dictated Step Coupling Polymerization"since the late 1980s.

本组自1984以来提出了利用&超分子化学调控的逐步偶联聚合反应&，合成了一系列梯形结构的聚硅氧烷。

Our group has prepared a series of ladderlike polysiloxane via "supramolecular chemistry-dictated step coupling polymerization"since the late 1980s.

本组自1984以来提出了利用&超分子化学调控的逐步偶联聚合反应&，合成了一系列梯形结构的聚硅氧烷。

This paper discusses design and realizable methods of remote test output interface from logical design angle.

本文从逻辑设计的角度讨论遥测输出接口的设计及实现方法。

This also 星体投射plies to buildings, structures and geological features.

这也适用于建筑物和地质特征。