盐酸安非他酮(bupropion hydrochloride)主要用于戒烟,治疗抑郁症.实验中将间氯苯丙酮作为起始原料,在双氧水-氢溴酸中进行溴化反应,合成中间体3'-氯-α-溴代苯丙酮.再进行胺化反应,得到安非他酮,浓盐酸酸化后得到粗品盐酸安非他酮.最后对粗品进行重结晶,获得成品.正交实验结果显示最优方案为反应温度40℃、反应时间16 h、溶剂类型为二氯甲烷.运用IR、HNM进行结构验证.按优化条件进行实验,操作简便,回收率高,产率为79.8％.

In order to find novel triazole lead compounds, a series of new triazole derivatives containing pyridine moiety were synthesized by the introduction of the important pyridyl backbone into the molecules of triazoles. They were structurally confirmed by H-1 NMR, C-13 NMR, IR, MS and elemental analysis. Additionally, compound 4k was structurally characterized through X-ray single crystal diffraction method. Preliminary bioassay data showed that some of the title compounds displayed moderate fungicidal and plant growth regulatory activities.

优化了以5-氰基苯酞为原料合成氢溴酸西酞普兰的技术方案,采用"一锅煮"法合并两步格式反应,经过水解、闭环、成盐反应,得到氢溴酸西酞普兰.改进后的制备过程温和易控,产品收率高,杂质含量低,适合工业化生产.

The target compound 3-(4-chlorobutyl)-1H-indole-5-carbonitrile was synthesized by 4 -hydrazinylbenzonitrile hydrochloride with 6 - chlorine hexanal adduct Sodiumbisulfite in the condition of polyphosphoric acid via Fischer indole cyclization.

Mitotane,an antineoplastic agent,was synthesized from 2-chlorobenzaldehyde by reaction with chloroform in KOH/CH3OH and DMF to give 2,2,2-trichloro-1-(2-chlorophenyl)ethanol,which was subjected to reduction followed by reaction with chlorobenzene in the present of sulfuric acid with an overall yield of about 27%.

AbstractThe synthesis of the novel title compounds (VI) and (VIII) with a biologically active thiazole moiety is presented.

(4,4-Dimethoxy-butyl)-dimethyl-amine,the structure ofwhich was identified by IR,MS and 1HNMR,was synthesized from tetrahydrofuran via a series of reactions including ring opening,oxidation,aldolization and substitution.Research shows that in this process conditions,simple and easy to control,the reaction process is polluteness and friendly to the enviroment,that the yield is high.

Twenty novel norcantharidin derivatives, which were substituted by thiazole ring, were synthesized in a single step by the [3+2] 1,3-dipolar cycloaddition reaction with oxime or hydrazone in the presence of chloramine-T when compared with the conventional method.

We use one molecule of ethylene diamine as a connecting arm to combine two molecules of 5,6-dehydronorcantharidin. Then, ten novel norcantharidin derivatives were synthesized in a single step by the [3 + 2] 1,3-dipolar cycloaddition reaction with oxime or hydrazone in the presence of chloramine-T, which is simpler than the conventional method.

Through 1,3-dipolar cycloaddition reaction,the novel pyrazole-linked norcantharidin derivative of substituted aromatic amines is obtained.The structures of the title compound are identified by 1HNMR,13CNMR and various two-dimensional nuclear magnetic resonance(NMR) spectra with some absorptions of 1H and 13C NMR assigned.Additionally,the configuration of the compound is elucidated.

旨在研究一系列5,6-去甲斑蝥酰亚胺衍生物的质谱裂解特征。研究结果显示异(口恶)唑并N-取代去甲去氢斑蝥酰亚胺衍生物,即各种1,3-偶极子氧化腈"现场"与N-取代斑蝥酰亚胺进行[3+2]环加成的系列产物在电子轰击下,质谱裂解的各种碎片呈现了此系列杂环分子结构环消除的规律性-逆1,3-偶极环加成反应的历程。

To design and synthesize disodium phosphate of novel norcanthridin analogues. All analogues have been screened for their antiproliferative activity in vitro against a panel of tumour cell lines: SMMC-7721, SGC7901, ECA109, A549 and MCF-7 producing IC50 values from 0.15 mu M to >50 mu M. Compounds 6 and 17 showed potency for the treatment of mammary adenocarcinoma, with IC50 value to MCF-7 cell line comparable to that of cantharidin, which proves that the phosphorylation of norcantharidin analogues is an effective way to increase the activity and solubility.

Fourteen new 1H-1,2,4-triazole derivatives containing pyridine moiety were synthesized by condensation of 1-(pyridine-3-yl)-2-(1H-1,2,4-triazol-1-yl)ethanone with aryl aldehydes, and their reaction conditions were studied. The title compounds were screened for their antibacterial and plant growth regulatory activities. The screening data revealed that most of the compounds showed some antifungal and plant growth regulatory activities. © 2007 Wiley Periodicals, Inc. Heteroatom Chem 18:376–380, 2007; Published online in Wiley InterScience (www.interscience.wiley.com). DOI 10.1002/hc.20308

Ten new 3-aryl-1-(pyridin-3-yl)-2-(1H-1,2,4-triazol-1-yl)prop-2-en-1-ols were synthesized by reducing 3-aryl-1-(pyridin-3-yl)-2-(1H-1,2,4-triazol-1-yl)prop-2-en-1-one with sodium borohydride. Their structures have been characterized by H-1 NMR and elemental analysis. Bioassay showed that some of them exhibited certain biological activities.

In search of potent 1 H -1,2,4-triazole derivatives with improving antifungal activity, a class of novel ferrocene–triadimenol analogues was synthesized and their biological potential evaluated. Screening data revealed that these new derivatives did not have the antifungal activities of parent compounds, but showed unexpectedly promising plant growth regulatory activity. Copyright © 2006 John Wiley & Sons, Ltd.

In the title compound, [Fe(C5H5)(C18H16N3O3)], the propene plane is tilted from its parent cyclopentadienyl ring by a small dihedral angle [17.9 (5)degrees], whereas the triazole and dimethoxyphenyl groups are nearly perpendicular to the propene plane [dihedral angles 75.9 (2) and 67.9 (2)degrees, respectively]. The cyclopentadienyl rings exhibit an almost eclipsed geometry.

In the title compound, [Fe(C 5 H 5 )(C 18 H 16 N 3 O 3 )], the propene plane is tilted from its parent cyclopentadienyl ring by a small dihedral angle [17.9 (5)°], whereas the triazole and dimethoxy­phenyl groups are nearly perpendicular to the propene plane [dihedral angles 75.9 (2) and 67.9 (2)°, respectively]. The cyclo­penta­dienyl rings exhibit an almost eclipsed geometry.

The title compound, C16H10Cl2N4O, has been synthesized as a potent fungicidal agent and plant growth regulatory agent, and its crystal structure was determined. In the crystal structure, weak intermolecular C-(HCl)-Cl-... interactions are found. The dihedral angles between the planes of the pyridine and triazole rings, and between the substituted phenyl and triazole rings, are 82.4 (2) and 118.8 (3)degrees, respectively.