苯并咪唑酮类镇痛新药重要中间体的合成研究(简报)

1999年底,日本万有药厂(Banyu Pharmaceutical Co.)开发出第一个选择性的非肽类的ORL1(opioidlike orphan receptor)受体拮抗剂J-113397.结果首次在中枢组织的ORL1受体证实,此化合物是具有高选择性、纯的、竞争性的ORL1受体抑制剂,且其药效极强,比通常的阿片受体(μ,κ,δ)的选择性高600倍以上.本文提出了一条合成J-113397重要中间体1-[1-环辛甲基-3-甲氧羰基-4-1,2,5,6-四氢吡啶基]-3-乙基-1,3-二氢-2H-苯并咪唑-2-酮的新路线(如图1).按照已报道的合成路线,作者未能获得苯并咪唑酮部分.于是本文以β-烯胺酯(10)为关键化合物,成功得到了苯并咪唑酮骨架.     

拟南芥bHLH家族转录因子DYT1在花药发育过程中调控胼胝质降解(英文)

胼胝质的合成和降解是雄配子体减数分裂过程中的一个重要特征,对后期花粉成熟有重要作用.在此研究中,分离到了一个雄性不育突变体msl57,该突变体的绒毡层分化及胼胝质降解过程出现异常,导致花粉败育.图位克隆和遗传分析表明:MSl57基因与bHLI-I家族转录因子DYTI(At4g21330)是同一基因.因此,将ms157突变体改名为dyt1-2.反式激活作用实验揭示了DYTI的激活功能域位于基因的250 ～504bp之间.通过酵母双杂交实验发现DYT1蛋白在体内可以形成同源二聚体来执行其功能.RT-PCR及定量PCR分析表明胼胝质酶相关基因A6的表达在突变体背景下严重下调.因此,DVF1通过调控胼胝质的降解来影响花药发育过程.     

2-甲基-2-硝基-3-戊烯-1-醇的制备

以甲醛，丙醛，硝基乙烷为原料，经过加成，脱水，羟烷基化，三步合成烯丙位硝基化合物2-甲基-2-硝基-3-戊烯-1-醇。总收率41．4％。     

CO2 regulator SLAC1 and its homologues are essential for anion homeostasis in plant cells

The continuing rise in atmospheric [CO2] is predicted to have diverse and dramatic effects on the productivity of agriculture, plant ecosystems and gas exchange. Stomatal pores in the epidermis provide gates for the exchange of CO2 and water between plants and the atmosphere, processes vital to plant life. Increased [CO2] has been shown to enhance anion channel activity proposed to mediate efflux of osmoregulatory anions (Cl- and malate(2-)) from guard cells during stomatal closure. However, the genes encoding anion efflux channels in plant plasma membranes remain unknown. Here we report the isolation of an Arabidopsis gene, SLAC1 (SLOW ANION CHANNEL-ASSOCIATED 1, At1g12480), which mediates CO2 sensitivity in regulation of plant gas exchange. The SLAC1 protein is a distant homologue of bacterial and fungal C4-dicarboxylate transporters, and is localized specifically to the plasma membrane of guard cells. It belongs to a protein family that in Arabidopsis consists of four structurally related members that are common in their plasma membrane localization, but show distinct tissue-specific expression patterns. The loss-of-function mutation in SLAC1 was accompanied by an over-accumulation of the osmoregulatory anions in guard cell protoplasts. Guard-cell-specific expression of SLAC1 or its family members resulted in restoration of the wild-type stomatal responses, including CO2 sensitivity, and also in the dissipation of the over-accumulated anions. These results suggest that SLAC1-family proteins have an evolutionarily conserved function that is required for the maintenance of organic/inorganic anion homeostasis on the cellular level.     

2/3场1-2-2区域紧逼防守战术解析

当代篮球运动对空间和时间的拼争更趋凶悍激烈,更加注重提高防守质量.全场区域紧逼防守由于综合了人盯人和联防的优点,且具有攻击性、破坏性,已被职业队广泛运用.由于全场区域紧逼防守对队员身体、技术、战术配合要求较高,而且全场防守范围大、体力消耗多、又易造成犯规,为了弥补战术的弱点、完善战术效果,在实践中派生出了全场区域紧逼防守的多种变形、换区阵型.2/3场1-2-2区域紧逼防守战术就是其中一种.这种战术继承了全场区域紧逼防守的核心内容———中场夹击、积极抢断,通过多年研究、实践证明,该战术适用于青少年业余比赛和训练,对促进技、战术的全面发展有着极其重要的作用.     

3-二氯乙酰基-2-甲基-2乙基-1,3-恶唑烷的合成研究

以ω（NaOH）＝33％水溶液为催化剂，乙醇胺，丁酮和二氯乙酰氯为原料，一步法合成了3－二氯乙酰基－2－甲基－2－乙基－1－，3－恶唑烷。采用正交实验设计获得最佳反应条件：苯作溶剂，反应温度0－－4℃，反应时间1h，产物收率78．6％，产品经红外光谱，核套共振和元素分析确证。     

丢番图方程(8a3-3a)2x +(3a2-1)y=(4a2-1)z

应用Bilu,Hanrot和Voutier关于本原素因子的深刻理论及二次数域类数的一些结果证明了丢番图方程(8a3-3a)2x+(3a2-1)y=(4a2-1)z仅有正整数解(x,y,z)=(1,1,3).     

丢番图方程(8a3-3a)2x+(3a-1)y=(4a-1)z

应用Bilu，Hanrot和Voutier关于本原素因子的深刻理论及二次数域类数的一些结果证明了丢番图方程(8a3-3a)2x+(3a2-1)y=(4a2-1)z仅有正整数解(x,y,z)=(1,1,3).     

人纤溶酶原K1—3区基因在大肠杆菌中的表达

将人纤溶酶原Krigle 1-3(K1-3)基因插入融合表达载体pET-17b,获得重组质粒pET-K13,转化E.coli BI21(DE3),在IPTG诱导下,人纤溶酶原K1－3基因在E.coli BI21(DE3,pET-K13)中获得高效融合表达,表达量占菌体总蛋白的24％,表达产物以包函体存在,Western blot证明重组 蛋白对人纤溶酶原抗血清有特异免疫原性。     

二苯甲醛叉丙酮-2,4-二硝基苯腙的合成以及对铜离子的识别

合成了新型荧光分子二苯甲醛叉丙酮2.4-二硝基苯腙,产物经IR、1H NMR和元素分析表征,通过了荧光光谱测定,结果显示其对铜离子有选择性识别作用。