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研究了脯氨酰肼有机小分子催化环己酮的直接α-硫代反应. 考察了3种不同硫代试剂、9种溶剂、6种脯氨酰肼催化剂等对反应的活性和收率的影响. 结果表明, 硫代试剂、溶剂及催化剂的结构对反应的活性和反应收率均有较大的影响. 在优化条件下, 即以邻苯二甲酰亚胺为硫代试剂, 甲苯为溶剂, 脯氨酰肼1和4催化的环己酮的硫代反应活性比较高, 室温反应12 h, 收率达98%. 脯氨酰肼催化该类反应条件温和, 操作简单, 在药物合成中具有一定的应用潜力. 相似文献
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N;N'-二(糖基硫代亚脲基)芳基硫代膦酰二胺的合成;糖基异硫氰酸酯;硫代膦酰二肼;生物活性 相似文献
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本文以低交联度的氯甲基化苯乙烯-二乙烯基苯共聚物与辛可宁,奎宁生物碱反应,合成了具有手性中心的相转移催化剂,并用它来诱导催化0-乙基硫代膦酰二氯与取代酚 的不对称缩合反应,合成了0-乙基,0-取代芳基硫代膦酰氯,为不对称合成有机硫代膦酰胺类化合物提供了一种新的方法,进行了一次有益的尝试。 相似文献
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利用O-烷基苯基硫代膦酸异硫氰基酯与胺的加成反应,合成了两系列O-烷基苯基硫代膦酰取代硫腺化合物。经元素分析、IR和1NNMR确定了它们的结构,并进行了除草活性的测试。 相似文献
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香草醛—N—酰腙类化合物的合成与表征 总被引:6,自引:0,他引:6
Schiff碱类化合物和酰腙类化合物大多具有除草,杀菌等生物活性,已有一些报道[1,2],对该类化合物的深入研究是当今农药界热点之一,表明此类化合物具有广阔的开发前景。据文献报道[1],香草醛与芳胺反应生成的Schiff碱类化合物具有优异的促进植物生根性。为寻求新的具有生物活性的物质,我们采用香草醛与酰肼反应,合成了3种未见报道的酰腙类化合物。其结构经IR,1HNMR和元素分析证实。合成反应如下:3—CH3O—4—HOC6H3CHO+H2NNHCO—R3—CH3O—4—HOC6H3CHNNHCO… 相似文献
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膦酰三胺类化合物具有优良的杀菌、抗病毒作用,其中部分还有抗肿瘤活性。脲和硫脲类化合物及其衍生物既具有优良的杀菌、除草等活性,又是一种重要的有机合成中间体。它的糖基衍生物是生物体内重要的代谢产物,具有维持代谢水平,提高机体耐受力等生理活性。糖基的多羟基特点,有利于增加这些化合物的水溶性, 相似文献
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采用水热合成方法得到3个新的双肼桥连过渡金属化合物:[M(N2H4)2Cl2]n(M=Mn(1),Ni(2)),{[Co1.5(N2H4)3PO4(H2O)]·H2O}n(3),用单晶X射线衍射方法对其晶体结构进行表征。化合物1是以2个肼分子桥联金属Mn和Ni形成1D链状结构,而粉末XRD显示1与2是同构的。化合物3是以2个肼分子桥联金属Co形成1D链,不同的1D链再通过磷酸根PO43-进一步堆积形成3D结构。磁性测试表明肼桥在磁性中心之间传递反铁磁耦合作用。 相似文献
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采用水热合成方法得到3个新的双肼桥连过渡金属化合物:[M(N2H4)2Cl2]n(M=Mn(1),Ni(2)),{[Co1.5(N2H4)3PO4(H2O)]·H2O}n(3),用单晶X射线衍射方法对其晶体结构进行表征。化合物1是以2个肼分子桥联金属Mn和Ni形成1D链状结构,而粉末XRD显示1与2是同构的。化合物3是以2个肼分子桥联金属Co形成1D链,不同的1D链再通过磷酸根PO43-进一步堆积形成3D结构。磁性测试表明肼桥在磁性中心之间传递反铁磁耦合作用。 相似文献
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YuXinLI YouMingWANG XiaoPingYANG SuHuaWANG ZhengMingLI 《中国化学快报》2004,15(1):14-16
The synthesis of 2-alkyl(aryl)-3-methylthiopyrano[4,3-c]pyrazol-4(2H)-ones via 5, 6-dihydro-2H-pyran-2, 4-dione-3-dithioacetals with (un)substituted hydrazines is described and the mechanism of the formation of title compounds is discussed. Their structures were confirmed by ^1HNMR spectra and elemental analysis. 相似文献
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《Journal of Saudi Chemical Society》2014,18(5):411-417
In the present investigation, a novel series of pyrazolines 2a–2d were synthesized by the cyclization of various -1-[2-(alkoxy) phenyl]-3-(thiophen-2-yl) prop-2-en-1-one 1a–1d with N-substituted phenyl hydrazine and thiosemicarbazide in the presence of CH3COOH and NaOH in ethanol which lead to the formation of new pyrazolines. The structures of these compounds were elucidated by, IR, 1H-NMR, 13C-NMR, ESI-MS spectral data and their purities were confirmed by elemental analyes. The in vitro antibacterial activity of these compounds was evaluated against two Gram-positive and two Gram-negative bacteria Aeromonas hydrophila, Yersinia enterocolitica, Listeria monocytogenes, and Staphylococcus aureus by microdilution method and then the minimum inhibitory concentration (MIC) of these compounds was determined. The results showed that compounds 1-[2-(benzyloxy) phenyl]-5-(thiophen-2-yl)-1-phenyl-4,5-dihydro-1H-pyrazol-4-yl (2b) and 1-[2-(naphthalen-2-ylmethoxy) phenyl]-5-(thiophene-2-yl)-1-phenyl-4,5-dihydro-1H-pyrazole-4-yl (2d) showed most promising antibacterial activity as compared to the antibiotics gentamicin and tetracycline in (Table 1, Table 2). 相似文献
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In continuing our efforts to find new effective antimicrobial agents for overcoming the problem of microbial resistance, a new series of functionalized 5-hetarylthiazoles have been designed and synthesized starting from readily accessible 1-(2-allylamino-4-methylthiazol-5-yl)ethanone (3). The structures of newly synthesized compounds were confirmed by elemental analyses, spectral data, and chemical transformations. The synthesized compounds were evaluated in vitro for their antimicrobial activity against some human pathogenic bacterial and fungal strains. The compounds 7, 18, and 24 exhibited higher antibacterial activity with minimum inhibitory concentration (MIC) values ranging from (0.03–0.06?µg/mL) than ampicillin (MIC, 0.12?µg/mL) against Streptococcus pneumoniae. Whereas compounds 4, 22, and 24 revealed higher antifungal potency than amphotericin B against Aspergillus fumigatus. The structure and antimicrobial activity relationship was also discussed. 相似文献
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P. Manivel F. Nawaz Khan 《Phosphorus, sulfur, and silicon and the related elements》2013,188(11):2910-2922
A series of hydrazinothiazoles has been synthesized by the condensation of thiosemicarbazones and α-bromoketones. Similarly the hydrazinothiazolidiones were prepared by the condensation of thiosemicarbazone and α-bromoesters. The newly synthesized compounds were characterized by NMR and LCMS studies. 相似文献