1H-吲唑-3-羧酸的合成

综述了1H-吲唑-3-羧酸的合成方法,并评述了其优缺点;同时介绍了作者在寻找其新合成方法中的一些探索。参考文献28篇。     

Synthesis of Isoquinoline-1, 3-Dicarboxylic Acid

Chiropticalluminescencemeasurementslhavebeenusedforstudyingchiralitydependentmolecularexcited-statedynamic,forstlldyingexcited-stateracemizationkineticsassociatedwithintermolecularchiralrecognitionprocessesinsolution2.Intheseprocesses,therearetwomolecularspecies,lanthanidecomplexes(luminophore)andresolvedtransitioncomplexes(AorA,quencher).Manykindsoftransitionmetalcomplexeshavebeenusedasquencherstoinvestigateinfluenceoftheintermolecularchiralrecognition.However,theluminophoreswereonlyconfined…     

Synthesis and Characterization of 3-Phenyl-adamantane-1-carboxylic Acid

Adamantane and its derivatives have been introduced into many drugs for current clinical research and some of them are used tor tlie treatment of neurological disease and/or used as the antiviral agents as well as the agents against type-2 diabetes.Recently,there have been many relevant research reported for developing medicinal chemistry by employing the adamantyl group.In this paper,a new adamantane-based compound (3-phenyl-adamantane-1-carboxylic acid,PACA) was synthesized and characterized by X-ray diffraction(XRD), themiogravimeric analysis(TGA),Fourier transtomi infrared spectroscopy(FTIR),etc.,which should be a beneficial complement or extension to the existing adamantyl-based materials.     

Synthesis and Crystal Structure of 3-（1-Ethyl-1H-indole-3-carbonyl）aminopropionic Acid

3-(1-Ethyl-1H-indole-3-carbonyl)aminopropionic acid has been synthesized by alkylation of 3-(1H-indole-3-carbonyl)aminopropionic acid methyl ester with bromoethane,follo-wed by saponifying and acidating,in 89.0% yield.Its crystal structure was gotten and determined by X-ray diffraction method.The crystal is of orthorhombic,space group P212121 with a = 8.9490(12),b = 11.1010(15),c = 13.0475(18) ,V = 1296.2(3) 3,Z = 4,Dc = 1.334 g/cm3,λ = 0.71073 ,μ(MoKα) = 0.095 mm-1,Mr = 260.29 and F(000) = 552.The structure was refined to R = 0.0306 and wR = 0.1445 for 2612 observed reflections with I 2σ(I).In the crystal structure,molecules are linked to each other through hydrogen bonds of N(2)-H(2)···O(1) and O(3)-H(3)···O(1),generating a three-dimensional network.     

一种制备(1R,3S)-3-氨基-1-环己烷羧酸的新方法

介绍了一种简单的制备(1R,3S)-3-氨基1环己烷羧酸的方法。以环己烷-1,3-二羧酸的顺反混合物为原料。经过关环得顺式的酸酐,然后酯化,在脂肪酶AY-30的作用下进行去对称性水解。得光学活性的环己烷-1,3-二羧酸的单乙酯产物,经过改进的Curtis重排反应后,羧酸基团转变为氨基。然后经过酯水解、去保护基团,得到光学纯的(1R,3S)-3-氨基-1-环己烷羧酸。     

3-溴-1-(3-氯-2-吡啶基)-1H-吡唑-5-甲酸的合成

以2,3-二氯吡啶为起始原料,通过水合肼亲核取代、马来酸二乙酯环合制得2-(3-氯-2-吡啶基)-5-氧-3-吡唑烷甲酸乙酯(5);5经苯磺酰氯酯化、溴化氢溴化制得3-溴-1-(3-氯-2-吡啶基)-4,5-二氢-1H-吡唑-5-甲酸乙酯(7);7经脱氢、水解合成了用于制备氯虫酰胺的关键中间体--3-溴-1-(3-氯-2-吡啶基)-1H-吡唑-5-甲酸,总收率39.5%,其结构经~1H NMR和MS确证.