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利用Hantzsch反应合成了13个N-芳基-4-(吡啶-2-基)-5-(1H-1,2,4-三唑-1-基)噻唑-2-胺衍生物,所有化合物的结构均经1H NMR,MS及元素分析确证.研究发现,溶剂对不同取代基的目标化合物的合成影响很大.生物活性测试结果表明,化合物均具有一定的杀菌活性.其中,化合物6c对番茄早疫和苹果轮纹、化合物6g对番茄早疫、化合物6h对黄瓜黑腥及化合物6i对苹果轮纹均显示80%以上的杀菌活性. 相似文献
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用叠氮钠和D-苯基甘氨酸为原料合成了2-[4-取代苯基-2-氧-3-酰氨基-1-吖啶基]-2-苯基乙酸类化合物. 在叠氮乙酰氯和亚胺化合物在三乙胺存在下在-78℃时进行环缩合反应, 可导致立体专一性合成顺-甲基-2-(4-取代苯基-2-酮-3-叠氮-1-吖啶基)-2-苯基乙酸, 催化氢化或硫化氢可减少叠氮基和得到氨基β-内酰胺后者被酰化生成α-酰氨基-β-内酰胺, 在温和碱性条件下选择性地氢化酯基既不会影响β-内酰胺环, 又不全影响酰胺侧链. 合成了二十个标题化合物, 其中九个被表明对β-内酰胺酶有抑制活性. 相似文献
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2-[二-(2-氯乙基)-胺基]-5-苄氧基-1,3,2-氧氮磷杂环己烷-2-氧化物是抗癌药物Endoxan的衍生物,其光学异构体的合成已有报道.本文报道了我们从廉价易得的手性原料天然-L-酒石酸开始,通过较为简捷的合成路线,完成了对目标化合物全部4个光学异构体的合成.化合物的有关数据参见表1. 相似文献
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为了研制航空燃料油的稳定剂,以脂肪酸1为原料,在三氯化磷存在下与溴反应,制得2-溴代脂肪酸2.化合物2在60~90℃石油醚中与氨基乙醇钠进行Williamson反应,盐酸中和,制得2-(2-氨基乙氧基)脂肪酸盐酸盐(3).以95%的乙醇为溶剂,在氢氧化钾存在下,化合物3与环氧氯丙烷反应后,冰醋酸酸化,合成了2-[2-(2,3-环氧-1-丙氨基)乙氧基]脂肪酸(4).化合物3和4均属新化合物. 相似文献
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3-甲基-5-苯砜基-3E-戊烯-1-醇(1)是合成某些萜类化合物的重要中间体.它具有反式烯丙基苯砜基双键.Julia等曾报道用含砜基的环丙基醇的开环重排反应来实现这类化合物的立体选择性合成,但其开环前体不易得到.本文以4-羟基-2-丁酮(2)为起始原料,经4步反应立体专一性地合成了标题化合物1.合成路线短、操作简便、易于大量制备.合成路线用方程式表示如下: 相似文献
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蛋白酪氨酸磷酸酶1B(PTP1B)作为胰岛素和瘦素信号转导通路的负调节因子,已成为治疗糖尿病和肥胖症的潜在靶标.为了寻找非磷酸酯类PTP1B抑制剂,设计、合成了一系列(E)-1-取代苯基-3-[4-((E)-(2-(4-苯基噻唑-2-基)腙)甲基)苯基]-2-丙烯-1-酮(4a~4n),并对化合物进行了PTP1B抑制活性测定.结果显示,所有化合物对PTP1B均显示出较强的抑制活性,其中化合物4h活性最佳,IC50为(2.57±0.50)μmol L-1. 相似文献
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Russian Chemical Bulletin - New 4-dimethylamino-2-(naphthalen-1-yl)-1-phenyl-1-(quinolin-3-yl)butan-2-ols with antituberculosis activity were synthesized.... 相似文献
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Hitherto unknown 3-(2H-Indazol-2-yl)-2H[1] benzopyran-2-ones (4a-f) have been synthesized under the trithyl phosphite (TEP) mediated reaction conditions of 3-[[(2-nitro-phenyl)-methylene]amino]-2H-1-benzopyran-2-ones (3a-f), obtained by the condensation of 3-amino coumarins (1a-f) with 2-nitro-benzaldehyde (2). 相似文献
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XU Liang-zhong LI Wei-hua YU Guan-ping QIN Yong-qi YANG Shuang-hua HOU Bao-rong 《高等学校化学研究》2005,21(5):528-530
In order to find leading compounds with an excellent fungicidal activity, the title compound 2-( 1,3-dithiolan-2- yl-idene)-1-phenyl-2-( 1,2,4-tfiazol-1-yl) ethanone was synthesized according to the biological isosterism and its structure was confirmed by means of IR, MS, ^1 H NMR and elemental analysis. The single crystal structure of the title compound was determined by X-ray diffraction. The preliminary biological test shows that the synthesized compound exhibits some biological activities. 相似文献
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[structure: see text] Oligonucleotides with novel modifications, 2'-O-[2-(amino)-2-oxoethyl] (2'-O-NAc), 2'-O-[2-(methylamino)-2-oxoethyl] (2'-O-NMAc), 2'-O-[2-(dimethylamino)-2-oxoethyl] (2'-O-DMAc), and 2'-O-[2-[[2-(dimethylamino)ethyl]amino]-2-oxoethyl] (2'-O-DMAEAc), have been synthesized. These modified oligonucleotides exhibit high binding affinity to complementary RNA (and not to DNA) and considerably enhance the nuclease stability of oligonucleotides with t(1/2) > 24 h. 相似文献
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DongMeiCAI MinJieLI DaLiangLI TianPaYOU 《中国化学快报》2004,15(2):163-166
Novel C-nucleosides of tiazofurin analogue (2-[2-(hydroxymethyl)-1,3-dioxolan-5-yl] 1,3-thiazole-4-carboxamide) and its thiol-substituted derivative (2-[2-(mercaptomethyl)-1,3-dioxolan-5-yl] 1, 3-thiazole-4-carboxamide) were synthesized from methyl acrylate through a multistep procedure. Their structures were confirmed by IR, ^1HNMR, ^13CNMR and elemental analysis. 相似文献
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2-萘基-5-取代苯并噁唑的合成、紫外光谱和萤光光谱 总被引:1,自引:0,他引:1
在研究有机化合物的结构与光性能间关系的过程中,我们又通过4-取代-2-氨基酚或其盐酸盐分别与α-萘甲酸和β-萘甲酸缩合,制得了十种2-(α-萘基)-5-取代苯并噁唑(Ⅰ)和十种2-(β-萘基)-5-取代苯并噁唑(Ⅱ),测定了这些化合物的熔点,紫外吸收光谱和萤光发射光谱. 相似文献
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Three sulfonated 1-(2-pyridylazo)-2-naphthols and six sulfonated 2-(2-pyridylazo)-1-naphthols were synthesized, and their application to the spectrophotometric determination of metals was studied. The acidity constants of the reagents and the stability constants of the nickel chelates are reported, and the relationship between their properties and the position of the sulfonic acid group is discussed. 1-(2-Pyridylazo)-2-naphthol-6-sulfonic acid (PAN-6S) and 1-(2-pyridylazo)-2-naphthol-7-sulfonic acid (PAN-7S) are sensitive and selective reagents for nickel. The determination of nickel in the presence of cobalt with PAN-6S is described. Extraction of the chelate as the ion-pair with tetraphenylarsonium ions into chloroform is suitable for the determination of 1–10 μg Ni at 570 nm; the molar absorptivity is 56 000 l mol-1 cm-1, and interferences are easily avoided. 相似文献