抗帕金森病药雷沙吉兰的合成工艺优化

以1-茚酮(1)为原料,在室温下与盐酸羟胺作用制得2,3-二氢-1H-茚-1-酮肟(2)。然后以乙醇作溶剂,经镍铝合金还原制得1-氨基茚满(3),并应用星点设计-响应面法对还原工艺进行了优化。随后再与对甲苯磺酸炔丙酯反应制得N-炔丙基-1-氨基茚满(4)。最后经L-酒石酸拆分、甲磺酸成盐得到雷沙吉兰(5)。以1为原料计算总收率约为31%。     

异香兰素化学合成的研究进展

异香兰素,化学名3-羟基-4-甲氧基苯甲醛,是一种非常重要的香料和食品药品领域应用广泛的医药中间体。近年来市场对异香兰素需求量不断增大,使得异香兰素的合成与应用研究也成为热点。简述异香兰素当前主要的应用状况,综述异香兰素不同的化学合成路线及进展,对各路线进行分析评价,展望利用生物技术、植物细胞培养技术等方法生产异香兰素的研究发展方向。     

Alcaligenes sp. CGMCC2428产威兰胶的分批发酵动力学模型

利用分批发酵研究Alcaligenes sp. CGMCC2428产微生物多糖威兰胶的合成特性,结果表明威兰胶的合成和菌体生长模型为部分偶联型.菌体和威兰胶质量浓度分别达到3.30和26.50 g/L,威兰胶对细胞干质量得率系数（YP/X）为8.20.根据分批发酵实验结果采用Logistic方程、Luedeking-Piret方程和Luedeking-Piret相似方程,得到了描述Alcaligenes sp. CGMCC2428生长、威兰胶以及葡萄糖底物消耗分批发酵动力学模型.同时改变初始葡萄糖质量浓度,实验数据与模型预测值进行了比较拟合,平均相对误差小于10%,表现出很好的适用性.     

三环酮的合成研究发展

本文简述了开瑞坦、去羧氯雷他定药物,并且综述其典型中间体三环酮的合成工艺路线.     

质子泵抑制剂兰索拉唑的合成

以2,3-二甲基-4-硝基吡啶-N-氧化物为原料,通过2个“一锅法”,经4步反应合成兰索拉唑.改进的合成路线缩短了合成工艺流程提高了产品收率,反应条件相对温和.总收率达到39.2％,高于文献报道的18.8％,适合工业化生产.     

3-乙氧基-4-甲氧基苯甲醛的合成

以乙醇为溶剂,以异香兰素和溴乙烷为原料,以碘化钾为催化剂,碳酸钾为缚酸剂,合成3-乙氧基-4-甲氧基苯腈中间体3-乙氧基-4-甲氧基苯甲醛。考察了原料摩尔比、反应体系的压力、反应温度及时间等因素对产品收率的影响。最佳合成工艺条件为:异香兰素45. 6g(0. 30mol),异香兰素与溴乙烷摩尔比为1. 00:1. 15,0. 5MPa下于85℃下反应5h,3-乙氧基-4-甲氧基苯甲醛的收率达到97%以上。     

用锆英砂合成锆石颜料的研究

本研究采用碱熔融法分解锆英砂,分解产物经氢卤酸处理后直接用于颜料的合成,合成的钒锆兰、镨锆黄和铁锆红颜料可以作为高温色釉的色料。     

雷替曲塞合成工艺综述

雷替曲塞被广泛用于治疗晚期结肠、直肠癌。按不同的起始原料对抗癌药物雷替曲塞的合成方法进行了总结。     

咪唑并[1，2-b]哒嗪

介绍了咪唑并[1,2-b]哒嗪的合成方法、用途、生产及需求.以3,6-二录哒嗪为原料,经氨化、环合、脱氯得咪唑并[1,2-b]哒嗪。咪唑并[1,2-b]哒嗪是合成头孢类抗生素的侧链中间体,因合成难度较大,成为国内开发头孢唑兰的瓶颈.     

印度兰的合成与应用

本文介绍了一种新型的酞菁钴染料印度兰的合成机理、工艺流程、检测方法及其产品的应用,并介绍了国内印度兰的发展现状和市场需求。     

New Peptide Functionalized Nanostructured Lipid Carriers with CNS Drugs and Evaluation Anti-proliferative Activity

Nanoparticulate systems have been widely investigated as delivery vectors for efficient drug delivery in different diseases. Nanostructured lipid carriers (NLC) are composed of both solid and liquid lipids (glyceryl dibehenate and diethylene glycol monoethyl ether) and have demonstrated enhanced biological compatibility and increased drug loading capability. Furthermore, the use of peptides, in particular cell-penetrating peptides, to functionalize nanoparticles and enhance cell membrane permeation was explored in this paper. In this paper, we described the synthesis of a new conjugated of tranylcypromine with MAP. In addition, taking into consideration our previous results, this study developed different NLCs loaded with three central nervous system (CNS) drugs (tacrine (TAC), rasagiline (RAS), and tranylcypromine (TCP)) functionalized with model amphipathic peptide (MAP) and evaluated their activity against cancer cells. Particle size analysis demonstrated NLC presented less than 200 nm and a polydispersity index less than 0.3. Moreover, in vitro results showed that conjugation of MAP with drugs led to a higher decrease in cell viability of a neuroblastoma cell line and Caco-2 cell line, more than MAP alone. Furthermore, NLC encapsulation contributed to higher cellular delivery and enhanced toxic activity at lower concentrations when compared with free or co-administration drug-MAP conjugate.     

Coumarin-Rasagiline Hybrids as Potent and Selective hMAO-B Inhibitors,Antioxidants, and Neuroprotective Agents

The frequency, complexity and morbidity of neurodegenerative diseases make them a great challenge for nowadays medicine. Most of the treatments currently used for Parkinson's disease – the second most prevalent – are only symptomatic. Therefore, it is urgent to develop drugs that are able to act simultaneously on different targets, being able to stop neuronal death and promote the recovery of neuronal populations already affected. In this work, we studied the activity of a series of hybrid molecules, which combine the structure of both coumarin and an alkynylamine group inspired on rasagiline, as MAO inhibitors, antioxidants and neuroprotective agents. Half of the studied hybrids turned out to be selective monoamine oxidase B (hMAO-B) inhibitors in the low micro/nanomolar range, demonstrating that positions 3 (compounds 1–3 ) and 7 (compounds 8 and 10 ) of the coumarin scaffold are the most suitable for the incorporation of the alkynylamine chain. All the studied compounds proved to be capable of neutralizing free radicals (DPPH). Finally, the 4-(but-2-yn-1-ylamino)coumarin ( 5 ) showed neuroprotective effects on glial cells and the 4-methyl-7-(pent-2-yn-1-ylamino)coumarin ( 8 ) inhibited intraneuronal ROS production as well.     

安克锰锌在荔枝树上施用的残留代谢消解规律与安全性评价

安克锰锌是烯酰吗啉两个异构体和代森锰锌组成的多元混合制剂。试样经粉碎、溶剂浸泡提取、混合柱净化,用气相色谱测定烯酰吗啉和代森锰锌母体(CS2),液相色谱测定代谢物乙撑硫脲(ETU)。仪器最低检出量:烯酰吗啉为1.436×10-12g,代森锰锌母体1.326×10-10g,ETU2.5×10-10g,最低检出浓度依次为0.02、0.025、0.02mg/kg,方法回收率依次为86.4%～90.8%、89.2%～95.9%、89.10%～95.13%;标准偏差为0.53～4.34;变异系数为0.58%～4.62%。安克锰锌在果皮中的消解方程广西和广东分别为C=1.2719e-0.1975T和C=1.045e-0.1972T,半衰期(T/2)均为3.5d;土壤中分别为C=0.8734e-0.1187T和C=0.6171e-0.1146T,半衰期(T/2)=6d;最高剂量250倍、最多施3次,最短距收期7d,在果肉中均未检出,果皮和土壤中的残留仅分别为0.1385～0.1745mg/kg和0.3105～0.3415mg/kg,均低于欧共体规定代森锰锌MRL值0.5mg/kg。     

Transcriptome Analysis Revealed the Embryo-Induced Gene Expression Patterns in the Endometrium from Meishan and Yorkshire Pigs

The expression patterns in Meishan- and Yorkshire-derived endometrium during early (gestational day 15) and mid-gestation (gestational days 26 and 50) were investigated, respectively. Totally, 689 and 1649 annotated genes were identified to be differentially expressed in Meishan and Yorkshire endometrium during the three gestational stages, respectively. Hierarchical clustering analysis identified that, of the annotated differentially expressed genes (DEGs), 73 DEGs were unique to Meishan endometrium, 536 DEGs were unique to Yorkshire endometrium, and 228 DEGs were common in Meishan and Yorkshire endometriums. Subsequently, DEGs in each of the three types of expression patterns were grouped into four distinct categories according to the similarities in their temporal expression patterns. The expression patterns identified from the microarray analysis were validated by quantitative RT-PCR. The functional enrichment analysis revealed that the common DEGs were enriched in pathways of steroid metabolic process and regulation of retinoic acid receptor signaling. These unique DEGs in Meishan endometrium were involved in cell cycle and adherens junction. The DEGs unique to Yorkshire endometrium were associated with regulation of Rho protein signal transduction, maternal placenta development and cell proliferation. This study revealed the different gene expression patterns or pathways related to the endometrium remodeling in Meishan and Yorkshire pigs, respectively. These unique DEGs in either Meishan or Yorkshire endometriums may contribute to the divergence of the endometrium environment in the two pig breeds.     

Responses to Odors of Dominant and Subordinate House Mice (Mus domesticus) in Live Traps and Responses to Odors in Live Traps by Dominant and Subordinate Males

Data from 16 0.1-ha field enclosures containing populations of wild house mice (Mus domesticus) were used to test two sets of questions. Do mice respond differentially to odors from dominant and subordinate males in live traps? Do dominant and subordinate males respond differentially to odors in live traps from other mice? A trap was considered odorized if it had captured a mouse during the previous week, during which there were always two trapping nights. Dominant and subordinate males did not differ with respect to the time they were alive in the enclosures, the frequency of capture, or home range size. Overall, mice were more attracted to the odor of dominant males compared to subordinate males. This difference was due primarily to the attraction of estrous and juvenile females to the traps odorized by dominant males. Dominant males were more likely to be captured in traps odorized by estrous females than in traps odorized by juvenile males or females, nonestrous females, or pregnant/lactating females. Subordinate males were caught more frequently in traps odorized by dominant males than were other dominant males. Conversely, dominant males were captured more frequently in traps odorized by subordinate males than were other subordinate males. Rates of capture of self-odor were higher for subordinate than for dominant males. The results may be explained by a combination of factors related to the social and reproduction systems of house mice.     

Study of oil soluble polymers as drag reducers

This investigation was undertaken to find the most effective material which would reduce the friction coefficient in turbulent flow when added in small quantities to oil pipelines. For this purpose, a series of oil-soluble polymers, namely homopolymers and copolymers of alkyl methacrylates, alkyl acrylates, and alkyl styrenes were synthesized. Emulsion polymerization techniques were used. Commercially available alkyl methacrylate and alkyl acrylate monomers were used in the synthesis. Monomeric alkyl styrenes were synthesized and structures established prior to polymerization. Intrinsic viscosities were measured and viscosity average molecular weights were calculated for several of the homopolymers synthesized in this study. Reduction of factional drag and resistance to shear degradation were measured by pumping a solution of the polymer in a hydrocarbon solvent through a pipe and recording the pressure drop across the pipe. Drag-reducing properties of several of the polymers were correlated in terms of their viscosity average molecular weights. Drag reduction of poly (isodecyl methacrylate) was studied in various hydrocarbon solvents. Drag-reducing behavior of polymers prepared in this study exhibited a strong dependence on molecular weight; increasing the molecular weight increased the drag reduction for a given polymer concentration and pipe size. Several of these polymers were found to be superior to commercially available polyisobutylene as drag reducers, especially in terms of shear stability.     

The effects of core material and cooling rate on fabrication defects in the veneer of bi-layered all-ceramic systems

The purpose of this study was to investigate the effects of framework thickness and cooling rate on the characteristics of fabrication defects in veneer ceramic of bi-layered lithium disilicate glass-ceramic (LDG) and zirconia. Eighty discs of 0.5-mm- and 1.0-mm-thick LDG/zirconia core were manually fabricated and veneered. Samples were divided into 8 groups according to the cooling rate, core material and core thickness, with 10 samples per group. All discs were scanned by micro-CT and 3D-reconstructed. Volume, position and sphericity of each pore defect were measured, and curves were fitted. Pore defect sizes of all samples were algorithm-fitted in two groups: 95% small defects and the rest large defects. Pore defects in veneer in LDG groups were smaller, rounder and farther from the interface with the core (p < 0.01), while large, irregular pores were observed at the zirconia interface. No differences in pore location or sphericity were found between the 0.5-mm- and 1.0-mm-thick samples in the LDG groups (p > 0.01), yet the pores in 1.0-mm-thick veneer in the zirconia core group were smaller, closer to the veneer surface, and rounder than in the 0.5-mm-thick group (p < 0.01). Pore defects in rapidly cooled samples in both LDG and zirconia frameworks were more irregular and closer to the interface with the core (p < 0.01). The pore defects were not only distinguishable between zirconia and LDG groups, but might also be related to their mechanical behaviors. The thickness of the core framework would influence the pore defect location as well as sphericity and was material-relevant. Cooling rate was deemed to be a factor in location and sphericity of pore defects in both LDG and zirconia core frameworks.     

2009年云南省昆明地区柯萨奇病毒B5的遗传特性分析

目的对2009年中国云南省昆明地区柯萨奇病毒B5(Coxsackievirus group B5,CVB5)的部分VP1基因序列进行分析,以了解CVB5的遗传特性。方法收集2009年中国云南省昆明地区临床诊断为无菌性脑炎患儿的200份粪便标本,设计针对CVB的通用引物,利用半巢式RT-PCR扩增部分VP1基因。PCR产物直接测序后,采用Omiga和Mega 5.05等生物学软件进行核苷酸、氨基酸序列及系统进化分析。结果共分离出7株CVB5,其部分VP1基因之间的核苷酸和氨基酸序列同源性均较高,分别为92.7%～98.5%和93.6%～100.0%;与中国其他不同地区参考株的核苷酸序列同源性为80.1%～99.1%,其中与中国山东株98388-SD-CHN-1998同源性较低;与中国其他不同地区参考株的氨基酸序列同源性为84.4%～100.0%,其中与中国河南株CoxB5-Henan-2010和中国山东株98388-SD-CHN-1998之间同源性最低;与其他不同国家参考株比较,其核苷酸和氨基酸序列同源性分别在77.5%～89.1%和92.1%～96.3%之间;与原型株Faulkner的核苷酸和氨基酸序列同源性分别为79.6%～80.9%和92.1%～95.4%。基因系统进化分析显示,分离的7株CVB5属于相对独立的1个分枝,中国流行株除98388-SD-CHN-1998外,构成1个分枝。结论 2009年中国云南省昆明地区CVB5流行株属于相同基因型。     

Solubilities and diffusion coefficients of carbon dioxide in poly(vinyl acetate) and polystyrene

Solubilities of carbon dioxide in poly(vinyl acetate) (PVAc) were measured at temperatures from 313.15 to 373.15 K and pressures up to 17.5 MPa. Diffusion coefficients of carbon dioxide in PVAc were also measured at 313.15 K and pressures up to 7 MPa. Solubilities and diffusion coefficients of carbon dioxide in molten polystyrene (PS) were studied at temperatures from 373.15 to 473.15 K and pressures up to 20 MPa. An apparatus using a magnetic suspension balance (MSB) was constructed for the measurements. The solubilities in the PVAc and the PS were in good agreement with literature data. The solubility in both polymers were correlated with the Sanchez and Lacombe equation of state to within an average relative deviation of 3.6 and 1.6% for PVAc and PS systems, respectively. The diffusion coefficients in PS were correlated with free volume theory of Kulkarni and Stern to within 10% of relative average deviation.     

Functionalized Hybrid Coatings on ABS Surfaces by PLD and Dip Coatings

It is important to give water-repellent and antibacterial properties to the acrylonitrile butadiene styrene (ABS) surfaces of the hearing aids. In this study, the sol–gel Si and sol–gel Ti solutions were prepared from the reactions of silicon ethoxide, titanium butoxide and methacrylic acid. The catalyst and Dynasylan F8815 were added to the sol–gel solutions to give hydrophobic properties onto the ABS surfaces. Additionally, silver nanoparticles were synthesized by nanosecond laser and added to the coating solutions to give extra antibacterial properties. The surfaces of the ABS targets were coated using the sol–gel dip coating and pulsed laser deposition techniques. The coatings with good adhesion between film and substrate and good water-repellent properties were achieved. The average contact angles for the coated ABS surfaces were measured in the range between 120 and 125 degrees. The obtained sol–gel materials and produced thin films onto the ABS surfaces were also analyzed in terms of the antibacterial properties. The highly antibacterial properties were observed in the sol–gel solutions and the thin films.