N-(1-(5-溴-2-((对氯苄基)氧基)苄基)-4-哌啶基)-N-乙基苯甲酰胺的合成及表征

以对氯苄氯、5-溴水杨醛为原料,通过消去、还原及溴化合成了4-溴-2-溴甲基-1-((4-氯苄基)氧)苯(Ⅲ),以1-苄基-4-哌啶酮合成了N-乙基-N-(4-哌啶基)苯甲酰胺(Ⅳ),通过Ⅲ、Ⅳ反应得到了一种新的非肽类CCR5拮抗N-(1-(5-溴-2-((对氯苄基)氧基)苄基)-4-哌啶基)-N-乙基苯甲酰胺,并对该产物进行了MS、13CNMR及1HNMR表征.     

N-(1-(5-溴-2-((4-氯苄基)氧基)苄基)哌啶-4-基)-3-氯-N-乙基苯甲酰胺的合成及表征

CCR5作为一种可利用的新靶点,用以防治人类HIV感染.以5-溴水杨醛、4-氯苄氯为原料,通过消去、还原及溴化合成了4-溴-2-溴甲基-1-((4-氯苄基)氧)苯(Ⅲ),以哌啶-4-酮为原料合成了3-氯-N-乙基-N-(4-哌啶基)苯甲酰胺(Ⅳ),通过Ⅲ、Ⅳ合成了一种新的非肽类小分子化合物CCR5拮抗剂N-(1-(5-溴-2-((4-氯苄基)氧基)苄基)哌啶-4-基)-3-氯-N-乙基苯甲酰胺,并对该产物进行了1HNMR、13CNMR及MS表征.     

N-烯丙基-N-(1-(5-溴-2-((4-氯苄基)氧基)苄基)-4-哌啶基)吡啶甲酰胺的合成及表征

趋化因子受体CCR5是HIV-1病毒进入人体细胞的主要辅助受体,CCR5拮抗剂可作为一种靶向制剂,以防治人类HIV-1感染.目前,非肽类小分子化合物CCR5拮抗剂的研究占据主导地位.以4-氯苄氯、5-溴水杨醛为原料,通过消去、还原及溴化合成了4-溴-2-溴甲基-1-((4-溴苄基)氧)苯(中间体3),以哌啶-4-酮合成了N-烯丙基-N-(4-哌啶基)吡啶甲酰胺(中间体7),通过中间体3和7合成了一种有望用作CCR5拮抗剂的非肽类小分子化合物N-烯丙基-N-(1-(5-溴-2-((4-氯苄基)氧基)苄基)-4-哌啶基)吡啶甲酰胺,该产物有一定的生物活性,并对该产物进行了1H NMR、13C NMR、IR及MS表征.     

N-哌啶基苯甲酰氨类CCR5拮抗剂的合成及表征

以5-溴水杨醛和4-氯苄氯为原料,通过消去、还原及溴化反应合成4-溴-2-溴甲基-1-((4-溴苄基)氧)苯(中间体Ⅲ),以1-苄基-4-哌啶酮合成2-氯-N-烯丙基-N-(4-哌啶基)苯甲酰胺(中间体Ⅶ),通过中间体Ⅲ和中间体Ⅶ合成新的非肽类小分子化合物N-烯丙基-N-(1-(5-溴-2-((4-氯苄基)氧基)苄基)-4-哌啶基)-2-氯苯甲酰氨,作为趋化因子受体(CCR5)拮抗剂,经GTPγS活性检测,其半抑制率IC50为(5.35±0.3)nmol/L,并对该产物进行1H NMR、13C NMR、IR及MS表征。     

4-甲基-N-烯丙基-N-(1-(5-溴-2-(对氯苄基氧基)苄基)-4-哌啶基)苯磺酰胺的合成及生物活性研究

以5-溴水杨醛、4-氯苄氯为原料,通过消去、还原及溴化合成了4-溴-2-溴甲基-1-((4-氯苄基)氧)苯(中间体3),以1-苄基-4-哌啶酮合成了4-甲基-N-烯丙基-N-(4-哌啶基)苯磺酰胺(中间体7),通过中间体3和7合成了一种新的非肽类CCR5拮抗剂4-甲基-N-烯丙基-N-(1-(5-溴-2-(对氯苄基氧基)苄基)-4-哌啶基)苯磺酰胺,并对产物进行了1 HNMR,13 CNMR,IR,MS表征及生物活性检测.结果表明,该拮抗剂合成总产率约为26.0%,具有较好的生物活性.     

N-烯丙基-N-(1-(5-溴-2-(对氯苄基氧基)苄基)-4-哌啶基)苯甲酰胺的合成及表征

趋化因子受体CCR5是HIV-1病毒进入人体细胞的主要辅助受体,CCR5拮抗剂可作为一种靶向制剂,以防治人类HIV-1感染.目前,非肽类小分子化合物CCR5拮抗剂的研究占据主导地位.本文以5-溴水杨醛、4-氯苄氯为原料,通过消去、还原及溴化合成了4-溴-2-溴甲基-1-((4-氯苄基)氧)苯(中间体3),以1-苄基-4-哌啶酮合成了N-烯丙基-N-(4-哌啶基)苯甲酰胺,通过中间体3、中间体7合成了一种有望用作CCR5拮抗剂的新的非肽类小分子化合物N-烯丙基-N-(1-(5-溴-2-(对氯苄基氧基)苄基)-4-哌啶基)苯甲酰胺,该产物有一定的生物活性,并对该产物进行了1 H NMR、13C NMR、IR及MS表征.     

溴代苯甲酰胺类拮抗剂的合成、表征及生物拮抗活性分析

非肽类小分子拮抗剂可以作为一种靶向制剂,用于防治人类HIV-1感染.溴代苯甲酰胺类非肽类小分子具有酰胺、哌啶、卤原子等活性基团而备受关注.该文合成了苯甲酰胺的邻位、间位以及邻位间位二取代溴化物中间体7,以对氯苄氯为原料合成了4-溴-2-溴甲基-1-((4-氯苄基)氧)苯(中间体3),通过中间体3、中间体7合成了3种新的溴代苯甲酰胺类拮抗剂8a-8c,对3种溴代物进行了1H NMR、IR、MS表征及生物活性检测.结果表明,N-烯丙基-N-(1-(5-溴-2-(4-氯苄氧基)苄基)-4-哌啶基)-2,5-二溴苯甲酰胺具有一定的生物活性.     

非肽类小分子拮抗剂苯甲酰胺衍生物的合成及表征

本实验以4-氯苄氯、5-溴水杨醛为原料,通过消去、还原及溴化合成了5-溴-2-(4-氯苄氧基)溴甲基苯(Ⅲ),以1-苄基-4-哌啶酮合成了N-丙基-N-(4-哌啶基)苯甲酰胺(Ⅳ),通过Ⅲ、Ⅳ合成了一种新的非肽类小分子化合物CCR5拮抗剂苯甲酰胺衍生物,对该拮抗剂进行了1H NMR、13C NMR及MS表征,同时,对产物进行了生物活性测试.     

4-哌啶基苯磺酰胺衍生物拮抗剂的合成及表征

趋化因子受体CCR5可作为一种可利用的新靶点,以防治人类HIV感染,非肽类小分子化合物CCR5拮抗剂的研究占居主导地位.本文以5-溴水杨醛、4-氯苄氯为原料,通过消去、还原及溴化合成了4-溴-2-溴甲基-1-((4-溴苄基)氧)苯(III),以1-苄基-4-哌啶酮合成了4-甲基-N-丙基-N-(4-哌啶基)苯磺酰胺(IV),通过III、IV合成了一种新的非肽类小分子化合物CCR5拮抗剂N-(5-溴-2-(对氯苄基氧基)苄基)-4-哌啶基)-4-甲基-N-丙基-苯磺酰胺,并对该产物进行了1H NMR、13C NMR及MS表征.     

甲基苯磺酰胺类CCR5生物拮抗剂的合成及表征

以1-苯甲基-4-哌啶酮合成了4-甲基-N-乙基-N-(4-哌啶基)苯磺酰胺(中间体7),以4-氯苯甲氯为原料,通过溴化及还原合成了5-溴-2-(4-氯苯甲氧基)溴甲基苯(中间体3),通过中间体7和中间体3合成了一种新的小分子化合物4-甲基-N-乙基-N-(N-(5-溴-2-(4-氯苯甲基氧基)苯甲基)-4-哌啶基)苯磺酰胺,对该产物进行了1 H NMR、MS、IR表征及生物活性检测,结果表明该化合物可以作为药物开发的候选化合物.     

Markedness and its Interpretation in Language Use

Language markedness is a common phenomenon in languages, and is reflected from hearing, vision and sense, i.e. the variation in the three aspects such as phonology, morphology and semantics. This paper focuses on the interpretation of markedness in language use following the three perspectives, i.e. pragmatic interpretation, psychological interpretation and cognitive interpretation, with an aim to define the function of markedness.     

Features of Women's language

Language is a means of verbal communication. People use language to communicate with each other. In the society, no two speakers are exactly alike in the way of speaking. Some differences are due to age, gender, statue and personality. Above all, gender is one of the obvious reasons. The writer of this paper tries to describe the features of women＇s language from these perspectives： pronunciation, intonation, diction, subjects, grammar and discourse. From the discussion of the features of women＇s language, more attention should be paid to language use in social context. What＇s more, the linguistic phenomena in a speaking community can be understood more thoroughly.     

Characterization of Ordovician carbonate reservoirs, southeastern Saskatchewan, Canada

The discovery of the prolific Ordovician Red River reservoirs in 1995 in southeastern Saskatchewan was the catalyst for extensive exploration activity which resulted in the discovery of more than 15 new Red River pools. The best yields of Red River production to date have been from dolomite reservoirs. Understanding the processes of dolomitization is, therefore, crucial for the prediction of the connectivity, spatial distribution and heterogeneity of dolomite reservoirs.The Red River reservoirs in the Midale area consist of 3～4 thin dolomitized zones, with a total thickness of about 20 m, which occur at the top of the Yeoman Formation. Two types of replacement dolomite were recognized in the Red River reservoir: dolomitized burrow infills and dolomitized host matrix. The spatial distribution of dolomite suggests that burrowing organisms played an important role in facilitating the fluid flow in the backfilled sediments. This resulted in penecontemporaneous dolomitization of burrow infills by normal seawater. The dolomite in the host matrix is interpreted as having occurred at shallow burial by evaporitic seawater during precipitation of Lake Almar anhydrite that immediately overlies the Yeoman Formation. However, the low δ18O values of dolomited burrow infills (-5.9‰～ -7.8‰, PDB) and matrix dolomites (-6.6‰～ -8.1‰, avg. -7.4‰ PDB) compared to the estimated values for the late Ordovician marine dolomite could be attributed to modification and alteration of dolomite at higher temperatures during deeper burial, which could also be responsible for its 87Sr/86Sr ratios (0.7084～0.7088) that are higher than suggested for the late Ordovician seawaters (0.7078～0.7080). The trace amounts of saddle dolomite cement in the Red River carbonates are probably related to "cannibalization" of earlier replacement dolomite during the chemical compaction.     

低渗透非均质砂岩油藏启动压力梯度研究

理论推导与室内实验相结合,建立了低渗透非均质砂岩油藏启动压力梯度确定方法。首先借助油藏流场与电场相似的原理,推导了非均质砂岩油藏启动压力梯度计算公式。其次基于稳定流实验方法,建立了非均质砂岩油藏启动压力梯度测试方法。结果表明:低渗透非均质砂岩油藏的启动压力梯度确定遵循两个等效原则。平面非均质油藏的启动压力梯度等于各级渗透率段的启动压力梯度关于长度的加权平均;纵向非均质油藏的启动压力梯度等于各渗透率层的启动压力梯度关于渗透率与渗流面积乘积的加权平均。研究成果可用于有效指导低渗透非均质砂岩油藏的合理井距确定,促进该类油藏的高效开发。     

On Tragic Consciousness In The Works By Ernest Hemingway

As an American modern novelist who were famous in the literary world, Hemingway was not a person who always followed the trend but a sharp observer. At the same time, he was a tragedy maestro, he paid great attention on existence, fate and end-result. The dramatis personae's tragedy of his works was an extreme limit by all means tragedy on the meaning of fearless challenge that failed. The beauty of tragedy was not produced on the destruction of life, but now this kind of value was in the impact activity. They performed for the reader about the tragedy on challenging for the limit and the death.     

A computer generator for randomly layered structures

AcomputergeneratorforrandomlylayeredstructuresYUJia shun1,2,HEZhen hua2(1.TheInstituteofGeologicalandNuclearSciences,NewZealand;2.StateKeyLaboratoryofOilandGasReservoirGeologyandExploitation,ChengduUniversityofTechnology,China)Abstract:Analgorithmisintrod…     

An Index mechanism for multi-scale view in spatial databases

There are numerous geometric objects stored in the spatial databases. An importance function in a spatial database is that users can browse the geometric objects as a map efficiently. Thus the spatial database should display the geometric objects users concern about swiftly onto the display window. This process includes two operations:retrieve data from database and then draw them onto screen. Accordingly, to improve the efficiency, we should try to reduce time of both retrieving object and displaying them. The former can be achieved with the aid of spatial index such as R-tree, the latter require to simplify the objects. Simplification means that objects are shown with sufficient but not with unnecessary detail which depend on the scale of browse. So the major problem is how to retrieve data at different detail level efficiently. This paper introduces the implementation of a multi-scale index in the spatial database SISP (Spatial Information Shared Platform) which is generalized from R-tree. The difference between the generalization and the R-tree lies on two facets: One is that every node and geometric object in the generalization is assigned with a importance value which denote the importance of them, and every vertex in the objects are assigned with a importance value,too. The importance value can be use to decide which data should be retrieve from disk in a query. The other difference is that geometric objects in the generalization are divided into one or more sub-blocks, and vertexes are total ordered by their importance value. With the help of the generalized R-tree, one can easily retrieve data at different detail levels.Some experiments are performed on real-life data to evaluate the performance of solutions that separately use normal spatial index and multi-scale spatial index. The results show that the solution using multi-scale index in SISP is satisfying.     

Jane Eyre——A Feminist In The 19th Century

In the 19th century the society was controlled by men, and women were just appendants of them, they had not any rights and freedom. But Jane was an exception, she showed some characteristics of early feminist. Jane showed her characteristics of feminism in three aspects: rebellion, equality, and independence. These characteristics were helpful to her success, and feminism is the only way out for women of that time.     

Achieving Unusual States of Matter Under High Pressure

正The periodicity of the elements and the non-reactivity of the inner-shell electrons are two related principles of chemistry,rooted in the atomic shell structure.Within compounds,Group I elements,for example,invariably assume the+1 oxidation state,and their chemical properties differ completely from those of the p-block elements.These general rules govern our understanding of chemical structures and reactions.Using first principles calcula-     

Exchange-Correlation and Electronic Excitation Energies from Pairing Matrix Fluctuations

We have developed an adiabatic connection to formulate the ground-state exchange-correlation energy in terms of pairing matrix linear fluctuations.This formulation of the exchange-correlation energy opens a new channel for density functional approximations based on the many-body perturbation theory.We illustrate the potential of such approaches with an approximation based on the particle-particle Random Phase Approximation(pp-RPA).This re-