Fine structure of 9-[2-(2-methylpyridin-5-yl)-ethyl]-1, 2,3,4-tetrahydro-γ-carbolines

On the basis of the results of PMR and mass spectra it has been shown that the pyridinyl-ethylation at the indole nitrogen atom of tetrahydro--carbolines in the protonated form gives rise to charge-transfer complexes. The UV spectra of the tetrahydro--carbolines and their pyridinylethylated analogs have been investigated.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 8, pp. 1050–1055, August, 1973.     

2-[5-(3,4,5-三甲氧基苯基)-1,3,4-噻二唑-2-基硫代]-1-(2,3,4-三甲氧基)苯乙酮肟醚合成与抗烟草花叶病毒活性研究

合成了4个2-[5-(3,4,5-三甲氧基苯基)-1,3,4-噻二唑-2-基硫代]-1-(2,3,4-三甲氧)苯乙酮肟醚新化合物, 并经过元素分析、红外光谱、核磁共振氢谱对其结构进行了表征. 初步生物活性测试表明, 化合物具有一定抗烟草花叶病毒活性.     

2-(1H-咪唑-1基)-1-(2,3,4-三甲氧基苯)乙酮的和成

联苯三醚;制备;2-(1H-咪唑-1基)-1-(2;3;4-三甲氧基苯)乙酮的和成     

Synthesis of (±)-2R,4R,5S-2-methoxy-4-nitro-5-(2,3,4-trimethoxyphenyl)cyclohexanone and (±)-2R,4S,5R-2-methoxy-5-nitro-4-(2,3,4-trimethoxyphenyl)cyclohexanone as colchicine mimetics

Colchicine mimetic (±)-4S,5R-4-nitro-5-(2,3,4-trimethoxyphenyl)cyclohexene (1) was epoxidized to afford a mixture of epoxides. The epoxides were separately converted in two steps, with high stereoselectivity, to two regioisomeric α-methoxyketones. One regioisomer, (±)-2R,4S,5R-2-methoxy-5-nitro-4-(2,3,4-trimethoxyphenyl)cyclohexanone (17), proved to be about 12-fold more potent than synthetic precursor 1 against HCT-116 tumor cells while the other regioisomer, (±)-2R,4R,5S-2-methoxy-4-nitro-5-(2,3,4-trimethoxyphenyl)cyclohexanone (16), and the synthetic intermediates tested showed no improvement in potency.     

(Z)-2-(1H-咪唑-1-基)-1-(2,3,4-三甲氧基)苯乙酮肟酯的设计与合成

三甲基苯乙酮肟;立体异构体;(Z)-2-(1H-咪唑-1-基)-1-(2;3;4-三甲氧基)苯乙酮肟酯的设计与合成     

Design,Synthesis, and Anticancer Evaluation of N-(4-{5-[4-(5-Methyl-1,3,4-oxadiazol-2-yl)phenyl]-4-(2,3,4-trimethoxyphenyl)-1,3-thiazol-2-yl}phenyl)benzamides

Russian Journal of Organic Chemistry - A series of substituted N-(4-{5-[4-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl]-4-(2,3,4-trimethoxy­phenyl)-1,3-thiazol-2-yl}phenyl)benzamides were designed...     

Identification and stereochemistry of (2s, 4s, 5r)- and (2r, 4s, 5r)-2,3,4-trimethyl-5-phenyloxazolidine, degradation products of ephedrine

The condensation of (−)-ephedrine with acetaldehyde gives two diastereomeric 2,3,4-trimethyl-5-phenyloxazolidines, of greatly differing thermodynamic stability. The structure and configuration of both the diastereoisomers was confirmed by chemical studies and by NMR spectroscopy.     

2-（1H-咪唑-1-基）-1-（2，3，4-三甲氧基）苯乙酮肟酯新化合物合成与生物活性研究

首次合成了12个2-（1H-咪唑-1-基）-1-（2，3，4-三甲氧基）苯乙酮肟酯新 化合物，并经元素分析、红外光谱、核磁共振氢谱对其结构进行了表征，初步生物 活性测试表明，有些化合物具有杀菌活性。研究了这些新化合物结构与光谱特征之 间的关系。     

2-(1H-唑基)-1-(2,3,4-三甲氧基)苯乙酮衍生物的合成与结构表征

首先以2－溴－1－（2，3，4－三甲氧基）苯乙酮，四丁基铵－1H－1，2，4－三唑或咪唑为原料，分别合成了2－（1H－1，2，4－三唑－1－基）－1－（2，3，4－三甲氧基）苯乙酮（Ia)和2－（1H－咪唑0－1－基）－1－（2，3，4－三甲氧基）苯乙酮（Ib)与盐酸羟胺反应生成2－（1H－1，2，4－三唑－1－基）－1－（2，3，4－三甲氧基）苯乙酮肟和1－（1H－咪唑－1－基）－1－（2，3，4三甲氧基）苯乙酮肟，产率为63％－72％，并经元素分析，IR和1H NMR进行了表征。     

4-Trifluoroacetamidobenzotriazole N2-2,3,4-tri-O-acetyl-β-D-ribopyranoside

4-Trifluoroacetamidobenzotriazole (I) was synthesized by acylation of 4-aminobenzotriazole with trifluoroacetic anhydride under mild conditions in pyridine. The silver salt (II) of I was obtained by treatment of base I with an aqueous alcohol solution of AgNO₃. Condensation of silver salt II with 1-bromo-2,3,4-tri-O-acetyl-D-ribopyranoside leads to 4-trifluoroacetamidobenzotriazole N₂-2,3,4-tri-O-acetyl--D-ribopyranoside (III). The structure of nucleoside III was confirmed by its IR, UV, and PMR spectra.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 12, pp. 1691–1692, December, 1978.     

2,3,4-三甲氧基苯基-苯基-烯酮与乙氧基乙炔的加成重排反应

研究了2,3,4-三甲氧基苯基-苯基-烯酮(9)与乙氧基乙炔的加成-重排反应, 得到2种薁酮异构体产物(11和12), 其结构经核磁共振波谱和X射线单晶衍射分析进行了确证. 该研究结果为Woodward所提出的分步反应机理提供了实验依据.     

N-(3-苯基2 ,3,4-三唑甲酰氨基)-N'-芳酰基硫脲及其环化产物的合成

以PEG 4 0 0为相转移催化剂 ,通过 2 苯基 1,2 ,3 三唑 4 甲酰基肼与芳酰基异硫氰酸酯的加成反应 ,合成了系列新的酰胺基硫脲衍生物 (3 ) ,3分别在酸性和碱性条件下环化制得相应的 1,3 ,4 噻二唑衍生物和 1,2 ,4 三唑啉 5 硫酮衍生物 ,并经元素分析、IR ,1HNMR和MS确证结构。     

Theoretical and experimental study on cyclic 6-methyl-2,3,4-tris(hydroxymethyl)pyridin-5-ol acetonides

Methods for the preparation of three cyclic 2,3,4-tris(hydroxymethyl)-6-methylpyridin-5-ol acetonides have been developed by variation of the reaction conditions. The six-membered acetonide turned out to be thermodynamically more stable than the seven-membered acetonide and bis-acetonide. The experimental data were consistent with the results of quantum-chemical calculations. The structure of the isolated compounds was proved by X-ray analysis.     

Cyclopropanation of 5-(allyloxymethyl)- and 5-(methallyloxymethyl)-5-ethyl-1,3-dioxanes with methyl diazoacetate

Reactions of 5-(allyloxymethyl)- and 5-(methallyloxymethyl)-5-ethyl-1,3-dioxanes with methyl diazoacetate catalyzed by Rh₂(OAc)₄ or Cu(OTf)₂ in the presence of [bmim]⁺Cl⁻, [bmim]⁺BF₄ ⁻, and [bmim]⁺PF₆ ⁻ proceed regioselectively at the C=C bond and lead to the formation of the corresponding cyclopropane-containing 1,3-dioxanes in yields up to 62%.