【摘 要】
:
Coumarins represent a class of synthetically useful heterocyclic compounds that have been accredited with a broad range of biological/pharmacological action such as antimicrobial,antifungal,antiviral,
【机 构】
:
College of Pharmacy and Institute of Medicinal Chemistry,Hubei University of Medicine,Shiyan 442000,
【出 处】
:
中国化学会第十六届全国有机合成化学学术研讨会
论文部分内容阅读
Coumarins represent a class of synthetically useful heterocyclic compounds that have been accredited with a broad range of biological/pharmacological action such as antimicrobial,antifungal,antiviral,anticoagulant,antitumor,and anti-inflammatory activities.Moreover,coumarin derivatives have the superior thermal stability and outstanding optical properties,including extended spectral responses,high quantum yields,and superior photostability.[1] On the other hand,heterocycles containing the oxazole nucleus also exhibit various biological and optical activities.[2] The introduction of a oxazole ring to the coumarin system is expected to influence the biological/optical activities significantly.Recently,we have been interested in the synthesis of fused pyrimidinones and imidazolones via aza-Wittig reaction,with the aim of evaluating their biological activities.[3,4]In our work,based on the structure of coumarin where there exists delocalization of π-electrons,a series of coumarin derivatives containing oxazole ring moiety were effectively synthesized by synthetic strategy of aza-Wittig reactions of functionalized iminophosphoranes(Fig.1).Furthermore,their structures are confirmed by by NMR,EI-MS,IR and elementary analysis.In addition,the optical properties including UV-vis/Fluorescence behavior performance are in progress.
其他文献
三元杂环中的氧杂环丙烷类化合物来源广泛,并且很容易转化成硫杂和氮杂环丙烷类化合物,因此,三元杂环类化合物是易得的合成子,通过扩环和开环反应,可以广泛用于有机合成中1.我们课题组最近基于三元杂环的扩环和开环反应实现了如下的合成转换.a)亲核性DABCO促进的氧杂环丙烷的Meinwald重排2a,b)有机酸碱促进的苯乙烯基氧杂环丙烷经串联反应制备联芳基甲醛2b,c)三氟化硼和d)有机酸碱促进的氰基氧杂
An efficient regio-and diastereoselective cyclization of sulfamate-derived cyclic imines with unsubstituted or monosubstituted α-halo hydroxamates is developed under mild conditions.This reaction proc
含硫有机磷化合物是有机农药的重要组成部分.硫-磷(S-P)键偶联反应是构建含硫有机磷化合物最为直接和有效的策略之一.到目前为止,有多个课题组报道了过渡金属催化硫-磷(S-P)键偶联反应,反应中使用的硫化合物多为硫醇、硫酚以及磺酰氯等气味难闻且毒性较大的原料1.基于绿色化学发展的理念,发展高效、低毒以及环境友好的合成策略构建硫-磷(S-P)键合成含硫有机磷化合物是当前碳-杂(C-X)键形成重要研究方
The genus Euphorbia are well-known medicinal plants for many kinds of deseases with long history in China.[1a] Among the numerous kinds of species,Euphorbia peplus has been used in traditional medicin
有机分子的精准官能团化是有机合成研究的重要方向,导向基诱导过渡金属催化的选择性碳氢键官能团化是强有力的工具之一.但其局限性在于需要额外的步骤来对底物进行预活化或者脱除导向基,从而降低了合成的效率.最新的策略是利用瞬态导向基可逆地和底物结合,实现位点选择性的惰性碳氢键官能化1.最近,我们通过加入催化量的氨基酸或苯胺衍生物与芳香醛或苯甲酰甲酸酯动态可逆形成亚胺,此亚胺通过双、单齿引导过渡金属钯、铱、钌
燕麦生物碱是由加拿大科学家Collins首次分离鉴定,并且命名为Avenanthramides,其中主要的三种是由Collins定义的燕麦生物碱A、B、和C.燕麦生物碱不仅有很强的抗氧化作用,而且具有止痒、抗增殖、抗炎等多种生物活性,对冠心病、结肠癌和皮肤瘙痒症的防治也起到了重要的作用,引起国内外学者的极大兴趣[1].近年来,国内外主要以皮燕麦为主要原料研究燕麦生物碱的含量、提取工艺及其生物活性等
对C-葡萄糖苷SGLT2抑制剂类化合物近端苯环的C6部位用不同官能团进行取代,在远端苯环上连接氮原子和体积较大的取代基,考察空间位阻对活性的影响.同时对合成过程中的反应时间、反应温度、反应溶剂、投料比等变量进行单因素筛选和优化,中间体2、4d和5d的产率分别达到了73.48%、72.38%和78.25%,目标化合物9c的产率达到了70.O9%.设计并合成了4个未见文献报道的新化合物,并通过核磁共振
The use of electron-rich cyclic(alkyl)(amino)carbenes(CAACs)as ligands in rhodium-catalyzed chemo-and stereoselective hydrogenation of aromatic ketones,phenols and boronated(hetero)arenes has been des
Cancer has been plaguing the history of human disease,and platinum complexes are classic anti-cancer drugs.However,platinum complexes have several disadvantages,including resistance,high toxicity,and
丙烯腈类杀虫剂对刺吸式口器害虫和咀嚼式口器害虫具有很好的防效,具有对作物安全、对蜜蜂及鱼类低毒的特点.1日产化学公司自1995年起对这类化合物进行了杀虫、杀螨等生物活性方面的研究,于2006年在专利中公开了具有高杀虫活性的新型丙烯腈类NC-510(图1),可以防治多种作物上的多种害虫.2-3本课题组近年来以NC-510为先导化合物,分别改变其单芳基(即A部分)、联芳基(即B部分)和酯基(即C部分)