2-(4-甲硫苯氧基)-3-(4-甲苯基)-4H-咪唑啉-4-酮衍生物的合成及杀菌活性(Ⅱ)

用烯基膦亚胺与4-甲苯基异氰酸酯、对甲硫苯酚的串联aza-Wittig反应合成了2-(4-甲硫基苯氧基)-3-(4-甲苯基)-4H-咪唑啉-4-酮衍生物.探讨了反应进行的条件和产物的波谱性质,提出了可能的环化反应机理.生成的环化产物均为新的化合物,其结构经元素分析、IR、1H NMR和MS确证.并探讨了所合成的新型杂环化合物的生物活性,结果表明部分化合物表现出良好的抑菌活性,其中3f的活性最好,在质量分数为5×10-5浓度时,对稻瘟菌和苹果轮纹菌的抑制率均达到100%.     

Synthesis and study of 4-(4'-n-alkoxybenzoyloxybenzoyl)-4'-n-butoxyanilides

Thirteen compounds with ester and amide linkages were synthesized and their mesogenic properties evaluated. Methyl to n-propyl derivatives exhibit nematic phases, n-butyl to n-decyl derivatives exhibit smectic and nematic mesophases, whereas n-dodecyl to n-octadecyl derivatives exhibit only smectic phases. All the smectic homologues exhibit smectic C phases. Middle members of the homologous series exhibit polymorphism of smectic mesophase. A plot of transition temperatures versus number of carbon atoms in the alkoxy chain reveals an odd-even effect for nematic-isotropic transition temperatures. Nematic-isotropic and smectic-cholesteric thermal stabilities of the prepared compounds (series I) are higher compared to those of previously reported compounds, series A, B and C. The results indicate that a simple reversal of a central linkage has a dramatic effect on the appearance of smectic mesophase in a homologous series. The structures of the synthesized compounds were characterized using elemental analysis, thin-layer chromatography and spectral data.     

(4S)-4-羧基杂氮硅三环的合成

利用L-N,N-双(β-羟乙基)丝氨酸及L-N,N-双(β-羟乙基)苏氨酸与三乙氧基硅烷或氯烷基三乙氧基硅烷反应合成了具有手性的(4S)-4-羧基杂氮硅三环(1～5),并运用IR、~1HNMR、EI-MS等手段表征了结构。证据显示存在着贯穿笼状结构的N→Si配键。     

1- and 2-(4-Hydroxycarbonylphenyl)-4-oxo-4,5,6,7-tetrahydroindazoles

Reactions of 4-hydrazinobenzoic acid with 2-formyl- and 2-acetyldimedones were utilized to synthesize 6,6-dimethyl- and 3,6,6-trimethyl-1-(4-hydroxycarbonylphenyl)-4-oxo-4,5,6,7-tetrahydroindazoles corre-spondingly, and the reaction with 2-cyano-3-ethoxy-5,5-dimethylcyclohex-2-en-1-one gave 2-(4-hydroxy-carbonylphenyl)-3-amino-4-oxo-6,6-dimethyl-4,5,6,7-tetrahydroindazole. Riga Technical University, Riga LV-1658. Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 4, pp. 516–519, April, 1997.     

One-Pot Three-Component Synthesis of a Series of 2-Amino-4-(4-oxo-4H-chromen-3-yl)-5-(2,2,2-trifluoroacetyl)-6-(trifluoromethyl)-4H-pyrans and 2-Amino-4-(4-oxo-4H-chromen-3-yl)-5-(thiophene-2-carbonyl)-6-(trifluoromethyl)-4H-pyrans as Promising Anticancer Agents

Russian Journal of Organic Chemistry - Novel functionalized 2-amino-4-(4-oxo-4H-chromen-3-yl)-5-(2,2,2-trifluoroacetyl)-6-(trifluoro­methyl)-4H-pyrans and...     

新型1-(4-氨基苯基)-4-(4-甲氧基苯基)哌嗪衍生物的合成

以二乙醇胺为原料,经溴化、环合、N-烷基化和还原4步反应制得关键中间体——4-[4-(4-甲氧基苯基)哌嗪-1-基]苯胺(4);4与酰氯经酰基化反应合成了11个新型的1-(4-氨基苯基)-4-(4-甲氧基苯基)哌嗪衍生物,其结构经1H NMR,FT-IR,ESI-MS和元素分析表征。     

Synthesis of substituted 2-ethyl-3-(4-hydrazinocarbonylphenyl)-4-quinazo-lones and 2-ethyl-3-(4-hydrazinocarbonylmethylphenyl)-4-quinazolones

Some substituted 2-ethyl-3-(4-hydrazinocarbonylphenyl)-4-quinazolones and 2-ethyl-3-(4-hydrazinocarbonylmethylphenyl)-4-quinazolones were synthesized and characterized by their sharp melting points, elemental analyses and spectral data.     

1-(4-氯苯胺基)-4-(4-吡啶甲基)-2,3-二氮杂萘琥珀酸盐的合成与抑制肿瘤活性

研究了1-(4-氯苯胺基)-4-(4-吡啶甲基)-2,3-二氮杂萘琥珀酸盐的合成工艺,采用苯酞和吡啶甲醛为起始原料,经加成、重排、取代和成盐4步反应得到目标化合物。 中间体及目标化合物通过1H NMR、MS和HPLC进行了表征。 重结晶纯化后的目标化合物纯度为98.1%。 对荷瘤（人大肠癌HT 29细胞）裸鼠的抑癌活性测定表明,该化合物具有明显的抑制肿瘤生长作用。     

4-(4-氨基苯基)-3-吗啉酮的合成

以乙醇胺为起始原料,通过环合、Goldberg藕联、还原,三步反应合成利伐沙班关键中间体4-(4-氨基苯基)-3-吗啉酮;该方法反应条件温和、生产成本低、绿色环保,具有良好的工业化前景。