Cyclization of 1,5-Hexadien-3-ols to 4-Halogeno-cyclohexenes: Obtention of Halogeno-Octahydronaphtalenes from Allyl-Pulegols.

TiCl₄ mediated cyclization of allyl-pulegols led to halogeno-naphtalenes.     

Synthesis of New 3-Phenoxypropan-2-ols with Various Heterocyclic Substituents

1-Phenoxy-3-piperidinopropan-2-ol, 1-(5-methyl-1,3-benzothiazol-2-ylsulfanyl)-3-phenoxypropan-2-ol, 1-(2-hydroxy-3-phenoxypropyl)azepan-2-one, 1,1′-(6-chloro-1,3-benzothiazol-2-ylimino)bis(3-phenoxypropan-2-ol), 1-(1,3-benzothiazol-2-ylsulfanyl)-3-phenoxypropan-2-ol, 1,1′-(piperazine-1,4-diyl)bis(3-phenoxypropan-2-ol), and 1,3-bis(2-hydroxy-3-phenoxypropyl)barbituric acid were synthesized by condensation of 1,2-epoxy-3-phenoxypropane with the corresponding amines and thiols.__________Translated from Zhurnal Organicheskoi Khimii, Vol. 41, No. 1, 2005, pp. 70–72.Original Russian Text Copyright © 2005 by Mesropyan, Ambartsumyan, Avetisyan, Galstyan, Arutyunova.     

固载计量氧化剂用于氧化反应

氧化剂固载化试剂,以其反应温和、选择性高、后续处理简单等环境友好特性,在有机合成反应中有着广泛应用.把各类氧化剂,如有机或无机态的Cr(Ⅵ)、Mn(Ⅶ)、MnO2和高价Fe与S、有机态I7 和I5 等,固载列氧化铝、硅胶、树脂、蒙脱石-KIO和分子筛等载体上,所形成的计量氧化剂可以选择性作用于醇类、硫醚、烯烃以及肟类化合物的氧化反应.     

Synthesis of Substituted 2-Azolyl-1-pyridylethan-1-ols

Through the reaction of (2-aryloxiran-2-yl)pyridines with triazole or imidazole a series of novel 2-azolyl-1-pyridylethan-1-ols has been synthesized with different positioning of the nitrogen atom in the pyridine fragment for pharmacological and agrochemical screening. The compounds prepared showed high fungicidal activity.     

Palladium-catalyzed tandem oxidative cyclization of 1-bromohexa-1,5-dien-3-ols: easy access to cyclopentenones

The novel Pd-catalyzed tandem cyclization of 1-bromohexa-1,5-dien-3-ols, prepared from the corresponding β-bromo-vinylaldehydes to cyclopentenone derivatives has been developed.     

Substituted 1,4-dicyclohexyl-butan-1-ols A new class of liquid-crystalline compounds

Abstract

1,4-dicyclohexyl-butan-1-ols with a lateral hydroxyl group in the middle part of the molecule exhibit higher clearing temperatures than those of the respective compounds whithout this lateral group. A smectic B-like texture and a low temperature additional phase X were found by microscopic and calorimetric investigations. A further unexpected result was the strong increase of the dielectric constant at the S_B/X transition. These preliminary results are explained in terms of hydrogen bridges.     

Substituted 1,4-dicyclohexyl-butan-1-ols A new class of liquid-crystalline compounds

1,4-dicyclohexyl-butan-1-ols with a lateral hydroxyl group in the middle part of the molecule exhibit higher clearing temperatures than those of the respective compounds whithout this lateral group. A smectic B-like texture and a low temperature additional phase X were found by microscopic and calorimetric investigations. A further unexpected result was the strong increase of the dielectric constant at the S_B/X transition. These preliminary results are explained in terms of hydrogen bridges.     

Palladium-catalyzed expedient Heck annulations in 1-bromo-1,5-dien-3-ols: Exceptional formation of fused bicycles

An unprecedented Pd-catalyzed intramolecular Heck cyclization has been investigated on halogenated diene scaffolds undergoing various mode of cyclization and termination leading to the formation of structurally differing fused cyclopenta(e)none and aromatic analogue. The discrimination in the fate of palladium intermediates formed in situ undergoing Heck cyclization preferentially arises out of the difference in reaction temperature as well as substrate architecture. Sequential Heck reaction of 1-Bromo-5-methyl-1-aryl-hexa-1,5-dien-3-ol derivatives followed by oxidation or termination via sp² CH activation in aromatic ring led to the formation of fused cyclopentanes. However, the similar reaction at elevated temperature showed predominance towards the formation of aromatic analogues via one pot cyclization and dehydroxylation. The mechanism for the formation of cyclopentanone fused with cyclopropane ring system is supported by density functional theory based calculations.     

Application of Polymer Supported Oxidants for the Selective Oxidation of Alcohols

Allylic alcohols can be successfully oxidized into the corresponding α, β-unsaturated aldehydes by two new types polymer-supported oxidizing reagents which do not oxidize saturated alcohols under similar condition.     

Efficient Room-Temperature Synthesis and Antimicrobial Study of Novel 2-Aroylbenzofuran-3-ols from Substituted Methyl Salicylates and Phenacyl Bromides

The article describes a convenient and efficient synthetic route for the construction of 2-aroylbenzofuran-3-ols from readily available diverse methyl salicylates and phenacyl bromides using K₂CO₃ as catalyst in dimethylformamide as solvent at room temperature. The reaction involves two steps, which occur in quick succession within 1 h to deliver the product with reasonably high yields. All the synthesized 2-aroylbenzofuran-3-ols (4a–u) were subjected for their antimicrobial studies, and some of these have shown prominent activity.

[Supplementary materials are available for this article. Go to the publisher's online edition of Synthetic Communications® for the following free supplemental resource(s): Full experimental and spectral details.]     

3-CH_2CH_2COOCH_3取代的1,5-苯并硫氮杂衍生物的合成、晶体结构及抑菌活性研究

从不同取代的苯出发,经5步反应合成了一系列3-CH2CH2COOCH3取代的1,5-苯并硫氮杂衍生物.化合物的结构经IR,1H NMR,13C NMR,MS和元素分析确证,并用X射线单晶衍射测定了化合物5f的晶体结构,证实了分子中的七元杂环是类船式构象.初步的抑菌活性测试结果表明,化合物5f和5h对枯草芽孢杆菌和临床新生隐球菌有微弱的抑制作用.     

Synthesis of 2-dialkylaminomethyltetrahydrofuran-3-ols

The reaction of esters of 4-R-3-methyl-2,3,4,5-diepoxyvaleric acids with secondary amines leads to the formation of esters of 4-R-5-dialkylamino-4-hydroxy-3-methyl-2,3-epoxyvaleric acids. The reduction of the latter with lithium tetrahydroaluminate and the cyclization of the reduction products in the presence of p-toluenesulfonic acid has given 2-dialkylaminoethyltetrahydrofuran-3-ols, the methiodides of which possess ganglion-blocking activity.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 11, pp. 1443–1446, November, 1973.     

基于清洁氧源的金属卟啉配合物仿生催化氧化研究进展

细胞色素P-450是光面内质网上的一类含铁的膜整合蛋白, 其核心结构是铁卟啉配合物, 它是生命体中P-450酶系的末端氧化酶[1]. 金属卟啉配合物作为细胞色素P-450酶活性中心的类似物, 因其能够在温和条件下, 高活性、高选择性地催化烃类、醇类等有机底物的氧化, 而受到人们的广泛关注[2].     

微波辐射促进的3-烷基取代咪唑并[1,5-a]吡啶合成

分别在常规加热和微波辐射条件下, 由双(2-吡啶甲酰)、二(2-吡啶)甲酮与脂肪醛及醋酸铵在醋酸溶剂中反应成功地制备了3-烷基取代的咪唑并[1,5-a]吡啶. 实验结果表明: 微波法比传统的合成方法产率高、反应时间短. 产物的结构经过¹H NMR, MS和元素分析表征.