共查询到20条相似文献,搜索用时 31 毫秒
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研究了一系列先前合成的喹喔啉化合物的抑制脂质过氧化活性,实验得到了这些化合物的体内和体外脂质过氧化抗氧化活性数据,发现这类喹喔啉化合物具有优异的抗氧化活性,其中,脂质过氧化清除率最高的化合物是2-(3-(3-甲氧基-4-羟基苯基)-2氧喹喔啉-1(2H)-烷基)乙酸,它在浓度为100μmol/L时,对应的清除率达到了57.7%。构效关系研究认为对羟基苯乙烯这一结构单元对于喹喔啉化合物在提高抗氧化活性有重要意义。 相似文献
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以1-乙基-3-(3-二甲胺丙基)碳二亚胺盐酸盐(EDCI)/1-羟基苯并三氮唑(HOBt)为缩合剂,5-氟尿嘧啶-1-基乙酸为中间体,分别与L-酪氨酸甲酯和D-酪氨酸乙酯通过液相偶联合成了(S)-2-(2-(5-氟-2,4-二氧-3,4-二氢嘧啶-1(2H)-基)乙酰氨基)-3-(4-羟苯基)丙酸甲酯和(R)-2-(2-(5-氟-2,4-二氧-3,4-二氢嘧啶-1(2H)-基)乙酰氨基)-3-(4-羟苯基)丙酸乙酯,水解后得到相应的酸对映体。所合成的化合物结构经1H NMR1、3C NMRI、R、MS及比旋光度等测试得以确证。四种化合物的体外抗肿瘤活性测试结果,说明该化合物的抗肿瘤具有一定的选择性,且R构型对抗肿瘤也起到了一定的作用。 相似文献
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介绍了头孢呋辛酸的侧链——— (Z) 2 甲氧亚氨基 2 (呋喃 2 基 )乙酸铵的结构和性质 ,及以呋喃乙酰和 2 呋喃 (羰基 )乙酸为起始原料的 3条不同的合成路线 ,得知以乙酰呋喃与亚硝酸进行肟化反应的路线是适合工业化生产的。最后简介了头孢呋辛酯 (钠 )的市场现状。 相似文献
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2-氯-5-(4-氯-1-甲基-5-三氟甲基-1H-吡唑-3-基)-4-氟苯甲醛是合成除草剂的中间体,它可以通过以下2步反应制得:首先,4-氯-3-(4-氯-2-氟-5-甲基苯基)-1-甲基-5-三氟甲基-1H-吡唑在乙酸/乙酐混合溶剂中用三氧化铬氧化,然后,在乙醇/水混合溶剂中,用碳酸氢钠催化水解得目的的产物,2步反应总收率达到71.6%。 相似文献
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Mahendra Yadav Sushil Kumar Laldeep Gope 《Journal of Adhesion Science and Technology》2013,27(11):1072-1089
Amino acid derivatives, namely, 2-(2-oxo-2-phenothiazin-10-yl)ethylamino)-3-mercaptopropanoic acid (OPEM) and 2-(2-oxo-2-phenothiazin-10-yl)ethylamino)acetic acid (OPEA) were synthesized and investigated as inhibitors for mild steel corrosion in 15% HCl solution using the weight loss, polarization, and electrochemical impedance spectroscopy (EIS) techniques. The inhibition efficiency of both the inhibitors increased with increasing the temperature and concentration of inhibitor. The inhibitors OPEM and OPEA show corrosion inhibition efficiency of 97.5 and 95.8%, respectively, in 200?ppm concentration, at 333?K. Polarization studies showed that both studied inhibitors were of mixed type in nature. The adsorption of inhibitors on the mild steel surface obeys Langmuir adsorption isotherm and the surface of inhibited and uninhibited specimens were analyzed by scanning electron microscopy (SEM). The semiempirical AM1 method was employed for theoretical calculations and the obtained results were found to be consistent with the experimental findings. 相似文献
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以氯乙酸甲酯、4-苯氧基苯酚为原料,在无水碳酸钾存在下,N,N-二甲基甲酰胺(DMF)为溶剂,制备了中间体2-(4-苯氧基苯氧基)乙酸甲酯(Ⅰ),进而,中间体(Ⅰ)和二甲胺反应。得到目的产物N,N-二甲基-2-(4-苯氧基苯氧基)乙酰胺(Ⅱ)。考察了反应温度、反应时间、物料投料比对目的产物(Ⅱ)收率的影响,从而确定了合成工艺条件为:反应温度15~20°C;反应时间3.5~4 h;物料投料比n(Ⅰ)∶n(二甲胺)=1.0∶1.4。在此条件下,N,N-二甲基-2-(4-苯氧基苯氧基)乙酰胺的收率达80%以上。化合物的结构经IR1、H NMR和元素分析进行了表征。 相似文献
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治疗艾滋病的沙奎那韦的中间体———(3S,4 aS,8 aS)-2〔-(2R,3S)-3氨-基-2羟-基-4苯-基丁基〕-N-叔丁基-十氢异喹啉-3-羧酰胺(Ⅱ)是通过(2S,3S)-4氯--3羟-基-1苯-基丁烷-2氨-基甲酸苄酯(Ⅲ)和(3S,4 aS,8 aS)-N-叔丁基-十氢异喹啉-3-羧酰胺(Ⅴ)反应得到的。该文对工艺进行了如下改进:Ⅲ的环化和与Ⅴ的反应合并为“一锅煮”工艺,去除原有文献报道的柱层析过程,只需洗去氢氧化钾的分液操作,直接加入w(Pd)=10%的Pd/C催化剂,室温反应12 h即脱去保护基。反应完毕后,以乙腈重结晶即得到目标产物Ⅱ。改进后的工艺总产率达到87%,w(Ⅱ)=98.5%。该法原则上适用于多种H IV蛋白酶抑制剂的合成。 相似文献
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以间溴苯酚和3-溴丙酸为原料,合成了间溴苯氧丙酸,并以间溴苯氧丙酸为原料,进一步合成了7-溴苯并二氢吡喃-4-酮。探讨了投料比、反应时间、反应温度、氢氧化钠的质量分数和加料顺序等因素对间溴苯氧丙酸收率的影响。适宜的反应条件为:n(间溴苯酚)∶n(氢氧化钠)∶n(3-溴丙酸)=1∶1∶1.3,反应温度95℃,氢氧化钠的质量分数8%,反应时间7 h,间溴苯氧丙酸收率71.4%。以间溴苯氧丙酸为原料,以85%的收率合成了7-溴苯并二氢唑喃-4-酮。 相似文献
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Anton S. Rudovich Miroslav Peina Anastasiya V. Krech Maria Y. Novozhilova Anastasia M. Tumilovich Tatyana V. Shkel Irina P. Grabovec Miroslav Kvasnica Luk Mada Maria G. Zavialova Arif R. Mekhtiev Radek Jorda Vladimir N. Zhabinskii Vladimir A. Khripach 《International journal of molecular sciences》2022,23(21)
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The syntheses and characterizations of poly [4-allyloxy-benzoic acid [4-(2-methoxy) ethoxy] biphenyl]-4-yl ester-co-4-allyloxy-[(4-cyano)-4-phenyl] carboxyl benzoate ester (poly [(MS3BDBE1)-co-(MCN)]x/y) (where x/y represents the molar ratio of the two structural units on the side chain) were performed in this study. The molar compositions of the structural units on the copolymers side chain were characterized by1H NMR. The transition temperatures, mesophase texture, and layer spacing (dl) of the polysiloxane polymers and copolymers were determined by differential scanning calorimetry (DSC), polarized optical microscopy, and X-ray diffraction patterns. The effects of the molar composition in the copolymers on the mesophase texture, transition temperatures, enthalpy/entropy change of mesophase/isotropic transition, dl of these copolymers were also discussed. 相似文献
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Mahmoud A. Abbady Hussein S. El-Kahef Mohamed A. Abd-Alla Maymouna M. Kandeel 《Journal of chemical technology and biotechnology (Oxford, Oxfordshire : 1986)》1984,34(2):62-72
Cyclonucleophilic addition of N-phthaloylaminoacid chlorides (II on 4-(N-ary-lideneamino)-4′-nitrodiphenyl sulphides (I) in dioxane and triethylamine afforded 4-(4″-aryl-3″-phthalylamino-2″-oxo-azetidin-1″-yl)-4′-nitro-diphenyl sulphides (III). Hydrazinolysis of III yielded 4-(4″-aryl-3″-amino-2″-oxo-azetidin-1″-yl)-4′-nitro-diphenyl sulphide hydrochlorides (IV). Condensation of IV with anisaldehyde using ethanol and piperidine as a basic catalyst gave 4-(4″-aryl-3″-anisylidine amino-2″-oxoazetidin-1″-yl)-4′-nitrodiphenylsulphides (V) in good yields. Interaction of V with chloroacetyl chloride in dioxane and triethylamine produced 4-(4″-aryl-3″-substituted β-lactamyl-2″-oxo-azetidin-1″-yi)-4′-nitrodiphenyl sulphides VI. Oxidation of IV, V and VI using hydrogen peroxide/glacial acetic acid mixtures gave the corresponding sulphones (VII), (VIII) and (IX). Sulphones of the type IX were obtained by unequivocal synthesis through interaction of sulphone-anils VIII with chloroacetyl chloride. The antibacterial activities of some of these compounds were determined. 相似文献