α-(5-氟尿嘧啶-1-基甲基甲酰基)氨基苯丙酸的合成

以5-氟尿嘧啶-1-基乙酸、二环己基碳二酰亚胺和L-苯丙氨酸为原料,1-羟基苯并三氮唑作为辅助试剂,通过碳二亚胺法合成了一种新型的α-(5-氟尿嘧啶-1-基甲基甲酰基)氨基苯丙酸,其结构经IR和元素分析表征.     

N~1羟烷基-5-氟尿嘧啶和α-5-氟尿嘧啶-N~1-二羧酸的研究

5-氟尿嘧啶(5-FU)是一种广谱性的抗肿瘤药物,其主要缺点是脂溶性小,口服吸收困难,毒副作用较大。为此,多年来,对5-FU进行了大量的化学修饰工作。已成功用于临床的5-FU衍生物主要有呋喃啶(FT-207),双呋喃啶(Thf_2-5-FU)、氟尿嘧啶脱氧核苷(FUDR)及卡莫氟(HCFU)等。在前文中,我们报道了1,3-二羟烷基-5-氟尿嘧啶和氨基酸短肽负载的5-氟尿嘧啶的合成及其抗肿瘤活性。     

新型氯苯基卟啉-5-氟尿嘧啶的合成

以3,4-二氯苯甲醛、对羟基苯甲醛,吡咯和1,5-二溴戊烷(或1,6-二溴己烷)为原料,经两步反应合成了溴烷氧基氯苯基卟啉(2a或2b);2与5-氟尿嘧啶反应,合成了两种新型的氯代苯基卟啉-5-氟尿嘧啶[1a(产率28.26%)和1b(产率29.34%)],其结构经UV-Vis,~1H NMR,IR和MS表征.     

聚5-氟尿嘧啶-1-乙酰天冬氨酰二胺的合成及其抗肿瘤活性

本文报道5-氟尿嘧啶-1-乙酰天冬氨酸,5-氟尿嘧啶-1-乙酰天冬氨酸双对硝基苯酯的合成。并用5-氟尿嘧啶-1-乙酰天冬氨酸双对硝基苯酯与一系列α,ω-二胺或赖氨酸乙酯缩聚,合成了五个聚5-氟尿嘧啶-1-乙酰天冬氨酰二胺和一个聚5-氟尿嘧啶-1-乙酰天冬氨酰赖氨酸乙酯。用~1HNMR,IR,UV和元素分析表征和签定了所得的单体和聚合物。抗动物肿瘤试验结果表明:聚5-氟尿嘧啶-1-乙酰天冬氨酰戊二胺,聚5-氟尿嘧啶-1-乙酰天冬氨酰赖氨酸乙酯,对小鼠艾氏腹水癌的抑制率分别为31.85％,44.23％。     

新型吡啶卟啉-5-氟尿嘧啶化合物的合成

新型吡啶卟啉-5-氟尿嘧啶化合物的合成;吡啶卟啉; 氟尿嘧啶; 合成     

5-氟尿嘧啶-β-环糊精前药的合成

为达到5-氟尿嘧啶结肠靶向释药的目的,合成了不同取代度的5-氟尿嘧啶-β-环糊精前药,其结构经UV-vis,1H NMR,13CNMR,IR,ESI-MS和元素分析表征.     

γ-核酸碱基取代丙基甲基二乙氧基硅烷的合成及其聚合反应研究

本文以Υ-溴丙基甲基二乙氧基硅烷分别与尿嘧啶、胸腺嘧啶、腺嘌呤和5-氟尿嘧啶进行烷基化反应,制得了四种含有核酸碱基或5-氟尿嘧啶的新型有机硅单体。通过它们的缩聚反应,合成了六种侧基含核酸碱基或5-氟尿嘧啶的聚硅氧烷。     

氨基酸5-氟尿嘧啶酯类衍生物的合成及其抗肿瘤活性研究

以N-保护的氨基酸钾盐与1-(ω-溴丙基)-5-氟尿嘧啶和1-(ω-溴丁基)-5-氟尿嘧啶反应,制备了18种氨基酸的ω-(N¹-5-氟尿嘧啶基)-丙醇酯和丁醇酯的盐酸盐,并确定了它们的结构。动物试验的初步结果表明,酪氨酸、苯丙氨酸的3-(N¹-5-氟尿嘧啶基)-丙醇酯盐酸盐对小鼠艾氏腹水癌的抑制率分别为88.1%和86.7%。     

新的4＇-去甲表鬼臼衍生物的合成及其抗癌活性

根据鬼臼毒衍生物和5-氟尿嘧啶的抗癌机理和构效关系,合成了7个新的4β-5-氟尿嘧啶取代4＇-去甲表鬼臼毒衍生物.在抑制金属基质蛋白酶I和胶原酶I活性测试中,化合物2.4和2.6的抑制活性比鬼臼乙叉甙(VP-16)和5-氟尿嘧啶(5-Fu)强3倍和5倍,在治疗癌细胞转移方面值得进一步探讨.     

5-氟尿嘧啶N1-甲酰基氨基酸、短肽的合成及抗肿瘤活性

5-氟尿嘧啶N¹-甲酰氯分别与Gly、Val、Leu、Ile、Phe、Asp和Glu的苄酯反应,制备了7种5-氟尿嘧啶-N¹-甲酰基氨基酸苄酯。氢解后得到了相应的5-氟尿嘧啶N¹-甲酰氨基酸。将其进一步与氨基酸甲酯或二肽甲酯缩合,制备了5-氟尿嘧啶N¹-甲酰基二肽甲酯和三肽甲酯。5-氟尿嘧啶-N¹-甲酰基二肽甲酯也可采用5-氟尿嘧啶-N¹-甲酰氯与二肽甲酯直接反应制备。     

5-氨基水杨酸锌及相关物质的高效液相色谱分析研究

对５－氨基水杨酸锌及相关物质５－氨基水杨酸、水杨酸、对氨基苯酚和５－苯偶氮基水杨酸的高效液相色谱法（ＨＰＬＣ）的分离条件进行了优化研究,结果表明,采用ＣＬＣ－ＯＤＳ（１５０ｍｍ×６．０ｍｍｉ．ｄ．,１０μｍ）作为分离柱,１％（Ｖ／Ｖ）ＨＡｃ－ＭｅＯＨ（４∶６）作为流动相,在流速为１ｍＬ／ｍｉｎ的情况下,上述５种物质在１０ｍｉｎ内可以达到基线分离,保留时间的日内和日间的变异系数分别小于２％和５％,在一定浓度范围内,浓度与峰面积的线性关系良好。     

SINGLE AND BINARY ADSORPTION PERFORMANCE OF SALICYLIC ACID AND 5-SULFOSALICYLIC ACID ONTO HYPERCROSSLINKED POLYMERIC ADSORBENTS

Single and binary adsorption behaviors of salicylic acid and 5-sulfosalicylic acid onto hypercrosslinked polymeric adsorbents, i.e. NDA-101 and NDA-99 were investigated. The Freundlich model can successfully describe all the adsorption isotherms tested, which indicates a favorable and exothermic adsorption process. The adsorption of salicylic acid relies on π-π interaction, while the electrostatic interaction further influences the adsorption of 5-sulfosalicylic acid onto NDA-99. The adsorptive capacity of salicylic acid on NDA-99 decreases but increases on NDA-101 with 5-sulfosalicylic acid as the background component in a binary solute system. The amount of 5-sulfosalicylic acid adsorbed was decreased with the increase in initial concentration of salicylic acid on both adsorbents. The competition for the adsorption sites is considered to be predominant in the solid-to-liquid interaction process. The adsorption selectivity of salicylic acid onto NDA-101 is higher than onto NDA-99 by more than an order of magnitude. Thus, combination technique involving NDA-101 followed by NDA-99 can be effectively applied to separate and recover salicylic acid and 5-sulfosalicylic acid from wastewater.     

MoCI_5在HZSM-5和APO-5上的负载及调变作用

MoCl_5在HZSM-5和APO-5上没有发生“双聚”,沸石的酸性对MoCl_5负载量的影响大于孔结构。APO-5负载MoCl_5后,仅生成数量和强度都很小的B酸中心。Mo-ZSM-5沸石在MTG反应中有Mo和Al的表面迁移,负载的MoCl_5通过氧化-还原及水解等过程产生羟基,增加了ZSM-5沸石的B酸量,通过B酸-L酸中心的电子协同效应增加载体的B酸强度,调变了催化剂的酸性分布。     

SURFACE ACIDITY OF ZEOLITE ZSM-5 AND ITS CATALYTIC PROPERTIES IN ESTERIFICATION OF ACETIC ACID WITH ALCOHOLS

IntroductionTheuseoflarge-PorezeolitessuchasXandYforcarelyzingtheesterificationhasbeenearlysuggestedbyBergklllandnorelationshipbetweentheactivityandsubdueaciditywasobserved.ItalianPatent[2]reportedthatdecationizedYzeolitesareveryactiveandselectivecatalyst…     

Electroanalytical behaviour of 5-nitroorotic acid

The electroanalytical behaviour of 5-nitroorotic acid has been studied at several pH values, using several techniques (DC and DP polarography and CV). The 5-nitroorotic acid undergoes five irreversible diffusion-controlled reduction waves over entire pH range considered. The optimum conditions for determination of 5-nitroorotic acid-with the above technique are also studied.     

Thiazolecarboxylic Acid Derivatives. 1. N-Substituted 2-Amino-4-methylthiazole-5-carboxylic Acid Derivatives

Acylation of the ethyl ester and anilide of 2-amino-4-methylthiazole-5-carboxylic acid gave 2-acetyl(arylsulfonyl)amino derivatives. Methylation of acetylaminothiazole and subsequent deacetylation gave 2-methylamino-4-methylthiazole-5-carboxylic acid, which was then converted into esters. The ethyl ester and anilide of thiazole-2-carboxylic acid were used as starting compounds for the synthesis of 2-dimethylaminoformimino- and 2-chlorobenzenesulfonylureido derivatives.     

KMnO4-乙二醛化学发光体系测定5-磺基水杨酸的流动注射分析

酸性介质下,KMnO4可以氧化5-磺基水杨酸产生化学发光,乙二醛对该体系有增敏作用。结合流动注射技术,建立了测定5-磺基水杨酸的流动注射化学发光方法。方法线性范围为2.0×10-8～2.0×10-5mol/L,检出限为2.0×10-9mol/L,对2.0×10-6 mol/L的5-磺基水杨酸平行测定11次,相对标准偏差为1.9%。该法可用于强力霉素废水中5-磺基水杨酸的测定。     

Expression and distribution of N-acetyl and N-glycolylneuraminic acids in secreted and cell-associated glycoconjugates by two human osteosarcoma cell lines

N-acetylneuraminic acid (Neu5Ac) and N-glycolylneuraminic acid (Neu5Gc) are the dominant sialic acids (Sia) in mammals usually found in the non-reducing terminal of oligosaccharide side chains in glycoproteins and glycolipids. Their expression and distribution pattern have been correlated both with the malignant phenotype and tumor grade of human cancers. The aim of the present study was to determine by reversed-phase HPLC method the amounts of Neu5Ac and Neu5Gc as well as their distribution among the culture media and cell surface of MG-63 and Saos-2 human osteosarcoma cell lines of high and low metastatic potential. It was determined that MG-63 cells produce up to 5-fold more total sialic acid as compared with the Saos 2 cells. Neu5Ac accounts for ca 60% of the total sialic acids secreted by MG-63 cells, whereas Neu5Gc is the predominant sialic acid present on the MG-63 cell membrane. Saos 2 cells secrete considerable amounts of Neu5Ac to culture media. The obtained data indicate that the human osteosarcoma cells express both forms of Sia-containing glycoconjugates; the differences in the amounts of each of the two major Sia types and their distribution may be related to their differences in morphology and/or metastatic potentials.     

Enhancing the Deactivation Durability of Nano-sized HZSM-5 for Aromatization by Adjusting its Ratio of Lewis/Brφnsted Acid Sites

Nano-sized zeolites have special physicochemical properties compared to micron-sized ones1,2. Recently, we have demonstrated the effectiveness and the remarkable deactivation durability of nano-sized HZSM-5 in converting the olefins of FCC gasoline to high octane number alkylbenzenes3. The role of zeolitic acidity is an intensively studied topic in the aromatizations of light hydrocarbons over micron-sized HZSM-5. But it is seldom reported for the aromatization of gasoline olefins over …     

Crystal Structure of Nicotinic Acid(3,5-dinitrobenzoic Acid Organic Adduct

The title compound nicotinic acid(3,5-dinitrobenzoic acid(NDNT)has been obtained by the reaction of nicotinic acid with 3,5-dinitrobenzoic acid in deionic water at room temperature.The crystal is of monoclinic,space group P21/n with a=14.053(6),b=5.046(2),c=20.105(8)A,β=103.573(8)°,C13H9N3O8,Mr=335.23,Z=4,V=1385.8(10)A3,Dc=1.607g/cm3,μ(MoKα)=0.137 mm－1,F(000)=688,R=0.0435 and wR=0.0993 for 1239 observed reflections (I>2σ(I)).In the crystals,the asymmetric unit contains one nicotinic acid (C6H5NO2)and one 3,5-dinitrobenzoic acid (C7H4N2O6)molecules which are linked by some hydrogen bonds to form a twenty-membered hydrogen-bonded ring and an extended linear structure.