2－杂萘满并喹啉的合成及抑菌活性的微量量热法研究

２－杂萘满并喹啉的合成及抑菌活性的微量量热法研究刘永军，丁养军，刘英（曲阜师范大学化学系曲阜２７３１６５）关键词２－杂萘满酮，抑菌活性，微量量热２－杂萘满酮具有（Ｉ）所示的化学结构，最常见的杂原子为Ｏ、Ｓ、Ｎ，关于Ｓｅ原子报道不多，分别俗称异色满酮、...     

异色满并吡唑衍生物的合成及其抗炎作用

异色满（isochroman）属于异革并毗哺类杂环化合物，近年来，已经合成出许多具有镇痛、降压、抗组胶和抗肿瘤等药理活性的异色满类化合物，但大都为异色满环上的1，2，4位取代衍生物或者螺环化合物［”’j，关于并杂坏的异色满报道甚少，鉴于许多有生理活性的天然产物中带有咄哩环以及异色满衍生物所表现的药理性质，本文选择异色满酮一4的足二酮衍生物为原料，完成了异色满并毗峻衍生物的合成，并对其抗炎活性进行了研究．合成路线如下：所用仪器有BRUCKER七0型核磁共振仪，TMS为内标；Perkin－Elmer1730型红外分光光度计，KBr压片；…     

异色满并含氮杂环类衍生物的合成

以异色满酮-4为起始原料，利用4-位羰基和α-位氢的缩合反应，合成出异色 满并吡啶、异色满并嘧啶、异色满并喹啉和异色满并萘啶类化合物，所合成的新化 合物均经核磁共振光谱、红外光谱及元素分析证明其结构．     

异色满并三氮杂酮化合物的合成

异色满(isochroman)是自然界中某些抗菌素和毒菌的基本骨架组成。例如,卡拉真菌素(kalafugin),七尾霉素(nanaomycin)和桔霉素(citrinin)等都是带有异色满环结构的杂环醌。近年来,人们合成了许多具有各种药理活性的异色满类化合物,其中引入异色满环的(艹卓)酚酮具有抑制肿瘤细胞的功能。为了合成类似活性的异色满类化合物,本文选择[1.2.4]三氮杂(艹卓)酮类的七员环系与异色满并环,旨在寻找抗癌新药。     

异色满酮-4及其衍生物的合成(Ⅳ)——辛可宁酸类似物的合成

由异色满酮-4(1)与邻氨基苯甲醛或邻氨基胡椒醛进行Friedlender缩合反应得到异色满并喹啉衍生物异色满并[4,3-b]喹啉(2)和9,10-亚甲二氧基异色满并[4,3-b]喹啉(3).     

异色满并[4,3—d]嘧啶类衍生物的合成

利用异色满酮－４合成了一系列新的异色满并嘧啶类衍生物４ａ－ｔｆ，其结构均经元素分析，ＩＲ和ＨＮＭＲ分析予以证实。     

异色满酮-4及其衍生物的合成(Ⅰ)

在异色满酮-4的合成中改变了介质,合成了异色满酮-4的五种O-酰基肟、六种Mannich碱、四种3-位亚甲基取代物和六种同嘧啶及吡唑并合的衍生物,并对于部分异色满酮-4的Mannich碱进行了药理试验。     

6,7—取代—1H—苯并（de）异喹啉—1,3（2H）二酮的合成

从二氢苊出发合成了６－溴－７－氨基２－（２′，４′－二甲基）苯基－１Ｈ－苯并（ｄｅ）异喹啉－１，３（２Ｈ）－二酮，６－甲氧基－７－氨基－２－（２′，４′－二甲基）苯基－１Ｈ－苯并（ｄｅ）异喹啉－１，３（２Ｈ）－二酮和６，７－二氨基－２－（２′，４′－二甲基）苯基－１Ｈ－苯并（ｄｅ）异喹啉－１，３（２Ｈ）－二酮，测定了它们的荧光量子产率，讨论了分子内重原子溴和给电子基对化合物荧光性质的影响。     

异色满酮—4及其衍生物的合成：Ⅹ.异色满并嘧啶并唑类杂环化合物的合成

通过异色满酮－４的克莱森缩合反应得到其α,β－不饱和衍生物,后者分别与３,５－二氨基－４－苯偶氮吡唑,３－氨基－１,２,４－三唑和２－氨基－苯并咪唑缩合,得到相应的四环和五环系列标题物。所合成的新化合物的结构均经元素分析,ＩＲ及＾１Ｈ ＮＭＲ确证。     

有机化学试题选登

有机化学试题选登一、完成下列反应二、合成１．自苯合成２－苯基吲哚２．自硝基苯合成６，６’联喹啉３．自丙二酸二乙酯及必要试剂合成２－甲基－４－异丙基１，３环己二酮４．自丙二酸二乙酯及必要试剂合成β－（３－环己烯基）丙酸５．自乙酰乙酸乙酯合成４－甲基－４...     

吲哚衍生物合成与应用的研究进展

综述了以苯胺衍生物(或硝基苯衍生物)为原料合成吲哚衍生物的方法和吲哚衍生物的应用。吲哚类化合物的合成方法主要有：Fischer合成法,苯胺衍生物合成法,硝基衍生物合成法和Nenitzescu合成法等。吲哚衍生物在制药、染料和香料等领域有重要应用。参考文献105篇。     

高效液相色谱法手性分离二茂铁衍生物

建立了4个单手性和3个双手性(含有手性中心和面手性)的二茂铁衍生物在Chiralpak IC(纤维素-三(3,5-二氯苯基氨基甲酸酯))和Chiralpak IE3(直链淀粉-三(3,5-二氯苯基氨基甲酸酯))手性固定相上的高效液相色谱分离方法。4个单手性二茂铁衍生物中有3个可以在Chiralpak IE3固定相上实现基线分离,另外1个则在Chiralpak IC手性固定相上实现基线分离。3个双手性二茂铁衍生物可在Chiralpak IC手性固定相上实现基线分离。研究表明,这两种手性固定相对二茂铁衍生物具有较好的手性识别作用,并且具有互补作用。这一研究结果可为手性二茂铁化合物的分离提供借鉴和参考。     

有机噻吩类衍生物作为电致变色材料*

噻吩类衍生物包括聚噻吩衍生物和齐聚噻吩衍生物。本文从有目的地设计、合成噻吩类衍生物的角度出发,探索了其作为电致变色材料的应用,综述了噻吩类衍生物作为电致变色材料的最新研究进展。     

Synthesis of well‐defined functionalized polymers and star branched polymers by means of living anionic polymerization using specially designed 1,1‐diphenylethylene derivatives

This article covers precise syntheses of well‐defined chain‐end and in‐chain functionalized polymers, multi‐functionalized polymers with a definite number of functional groups, star‐branched and graft polymers by recently developed methodologies using specially designed 1,1‐diphenylethylene (DPE) derivatives. The DPE derivatives include various substituted DPE derivatives with functional groups and their derivatives, DPE‐functionalized DPE derivatives, and well‐defined DPE‐functionalized macromonomers. The synthetic utility and importance of these DPE derivatives are described via such polymer syntheses.     

Design and synthesis of two triazonine-carbaldehyde derivatives using several chemical tools

Several triazonine-carbaldehyde derivatives have been prepared using different protocols; however, some require special reagents and conditions. The aim of study involved the synthesis of two triazonine-carbaldehyde derivative using testosterone or OTBS-testosterone as chemical tool. Triazonine-carbaldehyde derivatives were prepared by a series of reactions that involve the following: (1) synthesis of two nitrobenzamide derivatives by reaction of testosterone or OTBS-testosterone with p-nitrobenzoyl azide using Copper(II) as catalyst; (2) reaction of the nitrobenzamides with ethylenediamine to form two triazonine derivatives using boric acid as catalyst; (3) preparation of hexynyl-triazonine derivatives by the reaction of two triazonines 6-chlorohex-1-yne in basic medium; (4) reaction of hexynyl-triazonine derivatives with benzaldehyde to form two triazoninol analogs; (5) preparation of triazoninynal derivatives through oxidation of triazoninol analogs with dimethyl sulfoxide; and (6) synthesis of triazonine-carbaldehyde derivatives by the reaction of triazoninynal derivatives with hexyne-1 using Copper(II) as catalyst. The chemical structure of compounds was determined by spectroscopic and spectrometric methods. In conclusion, in this work were prepared two triazoninone derivatives using several chemical techniques, which are simple procedures and easy to handle.     

Synthesis of 2-phenylbenzofuran derivatives as testosterone 5 alpha-reductase inhibitor

A series of 2-phenylbenzofuran derivatives with a carbamoyl, alkylamino, or alkyloxy group at the 5 or 6 position of the benzofuran ring were synthesized and evaluated for rat and human testosterone 5 alpha-reductase inhibitory activities in vitro. Against rat enzyme, the carbamoyl derivatives had more potent inhibitory activities than the alkylamino or alkyloxy derivatives, and the 6-carbamoyl derivatives tended to be more potent than the 5-carbamoyl derivatives. Against human enzyme, the 6-substituted derivatives had more potent inhibitory activities than the 5-substituted derivatives. The 6-carbamoyl and 6-alkylamino derivatives tended to show stronger inhibitory activities against human type 1 enzyme than against type 2 enzyme, but they were not largely selective.     

Isothiazoles IX. Halogenation of 2-substituted-4-isothiazolin-3-ones

Bromination of 4-isothiazolin-3-ones, I, gave the 4-bromo derivatives, III, in good yields, while formation of 4,5-dibromo derivatives, IV, was much more difficult. In contrast, chlorination of I, even under mild conditions, gave primarily 4,5-dichloro derivatives, VI, and lesser amounts of the 4-chloro derivatives, V. Vigorous bromination of the 4-methyl analog of I gave the 5-bromo derivatives, VIII, whereas mild chlorination gave predominantly the 4,5,5-trichloro derivatives, X.     

环糊精衍生物在荧光分析中的应用进展（下）

本文介绍了环糊精衍生物开发概况及目前已或将商品化的环糊精衍生物的合成思路与方法．重点阐述环糊精在荧光分析中的增效作用机理和应用，及环糊精母体和衍生物分析特性的不同．较详细地详述了光活性基团修饰的衍生物的开发和发展远景     

DBU-Catalyzed, facile and efficient method for synthesis of spirocyclic 2-oxindole derivatives with incorporated 6-amino-4H-pyridazines and fused derivatives via [3+3] atom combination

3-Cyanomethylidene oxindole derivatives were prepared in excellent yields utilizing DBU-promoted Knoevenagel condensation of isatin derivatives with active methylene reagents. The isolated products were then reacted with azaenamines via a DBU-promoted Michael addition to yield spirocyclic 2-oxindole derivatives with incorporated 6-amino-4H-pyridazines and their fused derivatives.     

Acylation of some substituted 1,2,4-triazole-3-thiones

Acylation of some substituted 1,2,4-triazole-3-thiones in the presence of triethylamine gives N-substituted derivatives. S-Substituted derivatives, which are readily transacylated to the N-substituted derivatives on heating, are formed in the case of 4-phenyltriazolethiones in alkaline media. In the case of 4-allyltriazolethiones acylation in alkaline media gives only the N-substituted derivatives. Bromination of the acyl derivatives gives the disulfides.