吲哚-2-甲酸和(S)-吲哚啉-2-甲酸的合成和相互转化研究进展

吲哚-2-甲酸和(S)-吲哚啉-2-甲酸均是具有生物活性的天然产物和众多降压药的特征结构片段,报道了它们的合成及其相互转化研究进展.吲哚啉-2-甲酸可由吲哚-2-甲酸还原制得,其中(S)-吲哚啉-2-甲酸可由外消旋体拆分或通过不对称合成法制备,其中"手性源法"作为一种新出现的方法具有较好的前景.吲哚-2-甲酸可由Fischer吲哚合成法制备,或通过取代苯胺或苯甲醛制备,也可通过吲哚啉衍生物氧化脱氢制备,其中Fischer合成法仍具有较强的竞争力.     

2-羟基-5,6,7,8-四氢-5,8-亚甲基喹啉-3-羧酸的合成

5,6,7,8-四氢喹啉及衍生物是医药和农药的重要中间体。2-羟基-5,6,7,8-四氢-5,8-亚甲基喹啉-3-羧酸是合成HIF脯氨酰羟化酶抑制剂的重要中间体,其合成方法目前无文献报道。本文以降冰片烯为起始原料,经水合、氧化、缩合、环合和水解5步反应合成目标产物,总收率43.09%,结构经¹H NMR、 ¹³C NMR和MS确证。该路线具有原料廉价易得、操作简单、后处理方便且收率较高等优点,适合工业化生产。     

2-氨基-6,7-二甲氧基-喹啉-3-甲酸甲酯的合成

以3,4-二甲氧基苯甲醛为起始原料,经硝化、缩合和还原反应合成了2-氨基-6,7-二甲氧基-喹啉-3-甲酸甲酯,其结构经UV,1HNMR,IR和MS表征。     

N-Methylcarbazole-3-carboxylic Acid and Its Amides

N-Methylcarbazole-3-carboxylic acid was synthesized from N-methyl-2-amino-4-carboxydiphenyl-amine through the corresponding diazo compound by a modified Pschorr procedure. The acid was converted into N-methylcarbazole-3-carbonyl chloride which was treated with amines containing benzo- and aza-crown ether moieties, as well as with 3-(dimethylamino)propylamine, to obtain the respective N-substituted amides.     

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。     

3-芳基噻唑烷-4-酮-2-酰胺的合成及其抗肿瘤活性研究

合成了系列新的3-芳基噻唑烷-4-酮-2-酰胺衍生物,并测试了化合物抑制肿瘤细胞增殖活性.部分化合物对A-549和Hela肿瘤细胞有弱的细胞毒性,而对BGC-823没有抑制作用,表现出一定的选择性.其中,化合物7ad对A-549有较强的抑制活性(IC50=21.0μmol·L-1),与阳性对照顺铂的抑制活性(IC50=19.4μmol·L-1)相当.初步的构效关系表明化合物的立体结构可能对其抗肿瘤活性影响较大.     

3-氨基环己基甲酸和cis-3-氨基环己烯基-5-甲酸立体异构体的合成

通过手性胺拆分方法，从3-环己烯基甲酸出发分别合成得到了3-氨基环己基甲酸（ACHC）的四个立体异构体，以及cis-5-氨基-3-环己烯基甲酸（ACHEC）的二个立体异构体。     

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.     

3-氟-6-碘吡嗪-2-羧酸甲酯的合成及晶体结构

以3-氨基吡嗪-2-羧酸为原料，经酯化反应、亲电反应和重氮化反应合成了3-氟-6-碘吡嗪-2-羧酸甲酯（1），总收率62.34%，其结构经¹H NMR、¹³C NMR和MS确证，用X-单晶衍射法测定了化合物的晶体结构。结果表明：1（CCDC: 1986368）属单斜晶系，空间群C2/c，晶胞参数a=17.6566(5) Å, b=4.74850(10) Å，c=19.6368(6) Å，β=95.6540(10)°，V=1638.39(8) ų，Z=8，R_gt(F)=0.0173，wR_ref(F²)=0.0465，F(000)=1056，μ=3.885 mm^-1。      

Reaction of Reformatsky Reagents with Substituted Alkyl Esters of 2-Oxochromene-3-carboxylic Acid

Reformatsky reagents generated from alkyl esters of bromoacetic, -bromopropionic, -bromobutyric, and -bromoisobutyric acids react with alkyl esters of 6,8-dibromo-2-oxochromene-3-carboxylic acid to form alkyl esters of 6,8-dibromo-4-(1-alkoxycarbonylalkyl)-2-oxochromane-3-carboxylic acid.