2-甲基-6-对甲苯基-1,6-庚二烯的合成

以对甲苯乙酮(1)为原料,经烯醇硅醚化,Lewis酸催化Michael加成反应和Wittig反应,合成了新倍半萜烯化合物2-甲基-6-对甲苯基-1,6-庚二烯。     

2-甲基-6-对甲苯基-1,6-庚二烯的合成

以对甲苯乙酮(1)为原料, 经烯醇硅醚化, Lewis酸催化Michael加成反应和Wittig反应, 合成了新倍半萜烯化合物2-甲基-6-对甲苯基-1,6-庚二烯.     

合成二氢茉莉酮的一种新方法

茉莉酮和二氢茉莉酮是一类名贵香料,研究这类化合物的合成方法一直是人们感兴趣的问题。已有许多报道,其中包括甲基乙烯基酮和庚醛或1-硝基庚烷进行Michael加成得到1,4-二酮进行分子内缩合成的二氢茉莉酮。本文报道一种从甲基乙烯基酮和1-己烯经过2-己基-5-甲基-1,2-氧硼杂环戊烷中间     

有限场方法研究环丁烯-1,2-二酮衍生物的非线性光学性质

本文利用有限场/PM3方法计算了环丁烯-1,2-二酮衍生物的偶极矩、极化率、一阶超极化率和二阶超极化率, 说明这类化合物是很好的非线性光学材料。     

1-硝基-4-芳基-3-丁烯酮类化合物的合成方法研究

4-芳基取代丁烯酮类化合物可用于合成香料、电镀、杀虫驱虫等方面,因其结构特性还可作为药物合成的中间体。本文通过α-硝化的二硫缩烯酮与芳醛在碱的催化下发生缩合反应,并脱去硫环,得到一系列1-硝基-4-芳基-3-丁烯酮类化合物。本文利用新的合成方法向4-芳基取代丁烯酮的1-位引入了硝基,使该碳原子具有更强的活性,该类化合物目前鲜有报道,在有机合成方向将会有很大的研究空间。这种方法反应条件容易控制,产率极高,提纯方法简便。     

喹啉二酮类化合物的合成研究——形成双(二氢喹啉二酮基)甲烷的可能途径

我们曾用2-(3-甲基丁烯-2-基)丙二酸二乙酯与 N-取代芳胺在高温下环合,制备了一系列4-羟基-3-(3-甲基丁烯-2-基)二氢喹啉-2-酮类化合物.在此反应中除得到正常产物外,尚分离到若干副产物,最主要的副产物为3,3′-双(二氢喹啉-2,4-二酮基)甲烷.Young 等人曾对产生这类副产物的机理作过讨论,并提出如下途径:     

3-芳基戊二酰基双(4′-苯并-15-冠-5)的合成

苯甲醛和对氯苯甲醛在碱存在下分别与4′-乙酰基苯并-15-冠-5缩合,生成冠醚化查尔酮1a和1b。此二化合物作为中间体进一步与4′-乙酰基苯并-15-冠-5发生Michael反应,生成两种酮型双冠醚2a和2b。     

3-芳基戊二酰基双(4'-苯并-15-冠-5)的合成

苯甲醛和对氯苯甲醛在碱存在下分别与4'-乙酰基苯并-15-冠-5缩合, 生成冠醚化查尔酮1a和1b. 此二化合物作为中间体进一步与4'-乙酰基苯并-15-冠-5发生Michael反应, 生成两种酮型双冠醚2a和2b.     

无溶剂研磨法快速合成3-芳乙烯基-1,5-二酮类化合物的反应研究

在无溶剂条件下,α,β-不饱和醛与芳香酮在室温下研磨得到2,4-共轭二烯酮,随后,2,4-共轭二烯酮与过量芳香酮在Na OH存在下进一步发生Michael加成反应,快速而高效地合成了3-芳乙烯基-1,5-二酮类化合物.该法与传统的溶液法相比具有不使用溶剂和催化剂,反应条件温和,反应时间短,操作简便等优点.     

苯并噻唑 盐催化合成1,4-二羰基化合物

在苯并噻唑 盐和三乙胺存在下, 醛可以作为酰基负离子的合成等价物对α,β-不饱和酮进行Michael加成, 生成相应的1,4-二羰基化合物. 文中对 盐的制备, 催化反应条件及催化反应的机理进行了研究和讨论.     

Soluble and polymer-supported 2- and 3-benzylated furans for the preparation of α,β-ethylenic carbonyl compounds

Soluble and polymer-supported 2- and 3-benzylated furans were subjected to a sequence involving a Diels-Alder reaction with α,β-acetylenic carbonyl compounds, a Michael addition, and a subsequent retro-Diels-Alder reaction to yield olefinic compounds. On solid support, this traceless strategy is advantageous since pure compounds were released in the thermal cycloreversion step. The fur-2-ylated resin allowed a highly diastereoselective synthesis.     

Synthesis of fluorinated materials catalyzed by proline or antibody 38C2 in ionic liquid

The utility of reusable ionic liquid-proline (or aldolase antibody 38C2) reaction system, proceeding the aldol reactions, is described. Further, obtained α-chloro-β-hydroxy compounds were transformed to the optically active α,β-epoxy carbonyl compounds. The aldolase antibody 38C2-ionic liquid system was able to reuse in Michael additions and the reaction of fluoromethylated imines.     

Synthesis of coumarin based Knoevenagel-Ugi adducts by a sequential one pot five-component reaction and their biological evaluation as anti-bacterial agents

An efficient multicomponent synthesis of Ugi compounds comprising coumarin backbone has been achieved by employing one pot five component sequential Knoevenagel-Ugi reaction. This method offers the advantages of easy handling procedure, atom economy, mild reaction conditions and good yields of products. A molecular library was synthesized by changing the substituents on two of the independent starting materials. The synthesized compounds were also tested for anti-microbial activities and were found to be moderate to good anti-bacterial agents.     

Efficient microwave-assisted synthesis of fused benzoxazepine–isoquinoline derivatives via an Ugi reaction/tautomerization/intramolecular SNAr reaction sequence

A series of compounds containing the benzoxazepine-isoquinoline scaffold was synthesized in a one-pot procedure via an Ugi reaction followed by tautomerization reaction between the keto and enol forms and intramolecular nucleophilic substitution. The microwave-assisted strategy allowed the facile synthesis of a library of target compounds and is applicable to the construction of diverse libraries of related compounds for high throughput screening in medicinal chemistry.     

Revisiting Amadori and Heyns synthesis: Critical percentage of acyclic form play the trick in addition to catalyst

Amadori and Heyns reaction are landmark reactions of carbohydrate chemistry. Synthesis of simple Amadori and Heyns compounds are complicated by various factors and require tedious column chromatographic or ion chromatographic separations. Herein, we report an improved catalytic method based on classical synthetic method of Amadori and Heyns compounds in light of new understanding of a factor governing the reaction. By utilizing the improved catalytic method, we have accomplished several Amadori compounds of d-tagatose and also numerous other Amadori and Heyns compounds.     

Light-Driven Catalyst-Free Access to Phthalazines: Entry to Antiviral Model Drugs by Merging Domino Reactions**

We report the development of a metal-free four-step one-pot synthetic strategy to access high-value functionalized phthalazines using o-methyl benzophenones as starting compounds. Combining a light-mediated enolization of o-methyl benzophenones/Diels-Alder reaction domino process with a subsequent deprotection/aromatization domino reaction in one-pot leads to sustainable and efficient organic synthesis. The tangible advantages, i. e., absence of catalysts or additives, utilization of commercially available and/or easily accessible substrates, mild reaction conditions, simplicity, and single work-up procedure, make this combined process highly appealing for the direct construction of various 1-aryl-phthalazines. Importantly, in vitro bioactivity evaluation of these newly prepared heterocyclic compounds demonstrated a strong antiviral efficacy against major human pathogens like HCMV and SARS-CoV-2.     

An enantioselective organocatalyzed aza-MBH domino process: application to the facile synthesis of tetrahydropyridines

A chiral acid-base organocatalyst was found to promote an aza-MBH domino process between α,β-unsaturated carbonyl compounds and N-tosylimines to afford tetrahydropyridine derivatives with high enantioselectivity.     

Polyoxometalate-Based Compounds for Photo- and Electrocatalytic Applications

Photo/electrocatalysis of water (H₂O) splitting and CO₂ reduction reactions is a promising strategy to alleviate the energy crisis and excessive CO₂ emissions. For the hydrogen evolution reaction (HER), oxygen evolution reaction (OER), and CO₂ reduction reaction (CO₂RR) involved, the development of effective photo/electrocatalysts is critical to reduce the activation energy and accelerate the sluggish dynamics. Polyoxometalate (POM)-based compounds with tunable compositions and diverse structures are emerging as unique photo/electrocatalysts for these reactions as they offer unparalleled advantages such as outstanding solution and redox stability, quasi-semiconductor behaviour, etc. This Minireview provides a basic introduction related to photo/electrocatalytic HER, OER and CO₂RR, followed by the classification of pristine POM-based compounds toward different catalytic reactions. Recent breakthroughs in engineering POM-based compounds as efficient photo/electrocatalysts are highlighted. Finally, the advantages, challenges, strategies and outlooks of POM-based compounds on improving photo/electrocatalytic performance are discussed.     

Development of an unexpected reaction pathway for the synthesis of 1,2,4-trisubstituted pyrrolo[1,2-a]quinoxalines through palladium-catalyzed cascade reactions

1,2,4-trisubstituted pyrrolo[1,2-a]quinoxalines are synthesized through the multi-component reaction of 3-substituted 2-chloroquinoxalines, propargyl bromide, and excess secondary amines in the presence of a palladium copper catalytic system. This one-pot process provides an unexpected synthesis of new trisubstituted pyrrolo[1,2-a]quinoxalines by the introduction of two amine substituents onto the fused pyrrole rings in a single reaction procedure. The compounds formed are fully characterized by the analytical spectral data and X-ray analysis. A number of synthesized pyrrolo[1,2-a]quinoxaline derivatives are also screened against the three bacterial strains Micrococcus luteus, Pseudomonas aeruginos, and Bacillus subtilis. According to the results obtained, compounds 3b, 3c, and 3e are active against M. luteus, compounds 3b and 3e are active against Ps. Aeruginos, and only compound 3f is active against all the three bacterial strains.     

糖碳苷类化合物的合成方法研究进展

综述了近年来利用重排反应、W ittig反应、金属有机反应等方法合成糖碳苷类化合物的研究进展。参考文献30篇。