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1.
吲哚并[1,2-b]吲哒唑类化合物与三氟甲磺酸甲酯成盐,再与对二甲氨基苯甲醛偶联合成了3个新型吲哚并[1,2-b]吲哒唑三氟甲磺酸盐衍生物(3a~3c),其结构经NMR和IR表征.用MTT法检测了3对白血病细胞HL-60和K562的抗肿瘤活性,结果显示3具有良好的体外抗肿瘤活性.  相似文献   

2.
以咪唑并[1,2-b]哒嗪为原料,与N-碘代丁二酰亚胺在三氟乙酸/二氯甲烷中于室温进行碘代反应制得3-碘咪唑并[1,2-b]哒嗪(3);3与三甲基硅基乙炔在Pd(OAc)_2催化下经Sonogashira偶联反应制得3-三甲基硅基乙炔基咪唑并[1,2-b]哒嗪(4);4在碳酸钾作用下脱除三甲基硅基合成了3-炔基咪唑并[1,2-b]哒嗪,总收率61.2%,其结构经~1H NMR和HR-MS确证。  相似文献   

3.
利用各种碘代的靛红为底物,与氨基硫脲在水-二氧六环(体积比为5∶1)混合溶剂为反应介质,K_2CO_3为碱条件下,进行缩合反应,有效合成了一系列结构新型的碘官能团化的[1,2,4]三嗪并[5,6-b]吲哚-3-硫醇类化合物。所合成的目标化合物结构均通过波谱数据和元素分析得以确认。  相似文献   

4.
嘧啶衍生物的合成已有大量文献[1~4]报道,但是用氰基肉桂酸乙酯和硫脲作为原料合成4-氧-2-硫代六氢嘧啶类化合物,国内外尚未见报道. 超声辐射下进行的很多有机反应产率高,反应时间短,反应条件温和[5,6].近来我们尝试了在室温下利用超声辐射催化合成4-氧-2-硫代六氢嘧啶类化合物,得到了较好的结果.为了进一步研究该方法的适用范围和此类化合物的性质和用途,合成了一系列的4-氧-2-硫代六氢嘧啶类化合物.实验结果(表1)表明,该方法具有反应条件温和、反应时间短、收率高、操作简便等优点,为4-氧-2-硫代六氢嘧啶类化合物的合成提供了一条方便、快捷、有效的合成方法.  相似文献   

5.
介绍了在碘-二甲基亚砜(I_2-DMSO)促进作用下,通过Pictet-Spengler反应合成噻唑并[3',2':2,3]吡啶并[4,5-d]吡啶并[1,2-a]嘧啶酮(5)衍生物的合成方法.该反应的关键中间体2-(3-氨基-5-苯氨基噻唑-2-基)-4H-吡啶[1,2-a]嘧啶-4-酮(3),由2-氯甲基-4H-吡啶[1,2-a]嘧啶-4-酮(1)与N-苯基-N'-氰基-咪唑硫代碳酸钾(2)通过Thorpe-Ziegler异构化反应制得.该合成方法反应条件温和,操作简单,收率高.  相似文献   

6.
以6-硝基-1H-吲唑为原料,经氮原子甲基化、催化氢化还原、亲核取代以及烷基化反应制得关键中间体N(2′-氯嘧啶-4′-基)-N,1-二甲基-1H-吲唑-6-胺(5);5与芳香胺进行亲核取代反应合成了一系列新型取代氨基嘧啶衍生物——N-(2′-取代氨基嘧啶-4′-基)-N,1-二甲基-1H-吲唑-6-胺,其结构经1H NMR和MS表征.  相似文献   

7.
综述了近几十年来在医药和农药领域具有广泛用途的嘧啶并嘧啶类化合物的合成研究进展,介绍了三大类嘧啶并嘧啶类化合物的主要结构类型:嘧啶并[1,2-a]嘧啶类化合物、嘧啶并[4,5-d]嘧啶类化合物、嘧啶并[5,4-d]嘧啶类化合物的相关合成方法及新进展.  相似文献   

8.
发展了一种通过铑催化碳氢二氟烯丙基化/N-碘代丁二酰亚胺(NIS)介导的环化反应构建含氟3,4-二氢嘧啶并[1,6-a]吲哚-1(2H)-酮衍生物的方法.该方法具有反应条件温和、底物适用范围广等优点.该方法为构建用于发现药物的含氟杂环化合物提供了潜在的策略.  相似文献   

9.
异氰酸苯醇和N-[2-(4,6-二甲基)-嘧啶基]-羟胺(5)反应生成1-[2-(4,6-二甲基)-嘧啶基]-1-羟基-3-苯基脲(6)。化合物(6)在三乙胺存在下和氯甲酸乙醇反应生成2-[2-(4,6-二甲基)-嘧啶基]-4-苯基-1,2,4-噁二唑烷-3,5-二酮(1)。  相似文献   

10.
马旺  刘永亮  郭宝铭  钟为慧 《合成化学》2012,20(1):90-93,106
在微波辅助下,Baylis-Hillman加成物与4-氨基-6-氯嘧啶或2-氨基-噻唑反应,快速合成了两类嘧啶酮衍生物——3-取代-7-氯-4H-嘧啶[1,2-b]哒嗪-4-酮和6-取代-5H-噻唑[3,2-a]嘧啶-5-酮,收率81%~98%,其结构经1H NMR,13C NMR,IR和MS确证。  相似文献   

11.
Abstract

Fragmentation pathways of 14 organophosphorus compounds derived from diethyl spiro[pyrimidino[5,3][1,2]oxazole] phosphonates, diethyl (oxazolo[5,4-d]pyrimidine-4,6-dione)phosphonates, and diethyl (pyrimidino[4,5-b][1,4] oxazine)phosphonates were investigated by electron impact mass spectrometry (EI-MS). The intensity of the recorded molecular ion peaks showed various values depending on the nature of the compounds. Characteristic fragment ions were formed by successive loss of simple functional groups followed by decomposition of heterocycles connected to pyrimidine rings.  相似文献   

12.
A pyrimidin-2-thione derivative 2 was prepared and treated with 1,2-dibromoethane, chloroacetic acid and ethyl chloroacetate to give the alkylation products 3,4,9,5, respectively. Furthermore, the reaction of 2 with acrylonitrile and hydrazine hydrate yielded the pyrimidino[2,1-b]thiazine derivative 7, and [1,2,4]-triazolo[4,3-a]pyrimidine 8. Compound 9 was used as the key starting material for synthesis of thiazolo[3,2-a]pyrimidine and pyrano[2′,3′ :4,5]thiazolo[3,2-a]pyrimidine derivatives 10–13, through the reaction with ethyl acetate, malononitrile, hydrazine hydrate, β-aroylacrylic acid, and chalcone, respectively. Treatment of compound 5 with 3,5-dibromo-2-aminobenzoic acid in refluxing butanol gave the 3,1-benzoxazinone derivative 6. The structure assignment of the new compounds is based on chemical and spectroscopic evidence.  相似文献   

13.
2-Methyl-4-aryl-5-oxo-4,5-dihydro-1H-indeno[1,2-b]pyridine derivatives react with methyl iodide in an aprotic medium in the presence of alkaline agents to give C- and N-alkylation products, viz., 2,4a-dimethyl- and 1,2-dimethyl-4-aryl-5-oxo-4,5-dihydroindeno[1,2-b]pyridines, and with dimethyl sulfate or methyl p-tosylate under the same conditions to give N-methylation products.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 3, pp. 393–398, March, 1984.  相似文献   

14.
Several derivatives of the pyrido[1',2':1,2]pyrimido[4,5-b]indoles 4 and the pyrazino[1',2':1,2]pyrimido[4,5-b]indoles 14 were synthesized by treatment of the benzannulated enyne-isocyanates 8 with the iminophosphoranes 9 and 13, respectively, for the aza-Wittig reaction followed by thermolysis. The reaction presumably proceeds through an initial formation of the corresponding benzannulated enyne-carbodiimides, such as 10, followed by a formal intramolecular hetero Diels-Alder reaction. Surprisingly, when the iminophosphorane 17 was used for condensation with 8, the expected pyrimido[1',6':1,2]pyrimido[4,5-b]indoles 16 were not obtained. Instead, the isomeric pyrimido[6',1':2,3]pyrimido[4,5-b]indoles 21 were isolated. Presumably, an alternative reaction pathway involving an initial [2 + 2] cycloaddition reaction to form 19 followed by ring opening could lead to 20 and, after an intramolecular radical-radical coupling, 21. Treatment of the urea derivatives 24 with dibromotriphenylphosphorane also produced in situ the benzannulated enyne-carbodiimides 25, which on thermolysis gave the isoquinolino[2',1':1,2]pyrimido[4,5-b]indoles 26. Methylation of 4a, 14a, and 26a with methyl iodide occurred exclusively at the site of the indolo nitrogen. The planar geometry of those novel heteroaromatic compounds, resembling many DNA-binding agents, makes them potential candidates as DNA intercalators.  相似文献   

15.
N-Acylbenzotriazoles react with aryl isocyanates to form, depending on the type of acyl group, compounds based on five different classes of polycyclic heteroaromatics. Higher alkanoyl-, acetyl-, acetoacetyl-, aroyl-, and cinnamoylbenzotriazoles yield, respectively, derivatives of quinoline, pyrimidino[5,4-c]quinoline, benzo[b]-1,8-naphthyridine, phenanthridine, and indolo[2, 3-b]quinoline by incorporating 3, 3, 4, 2, and 2 molecules, respectively, of the isocyanate per acylbenzotriazole molecule.  相似文献   

16.
[reaction: see text] Phenylene-linked bisnaphthopyrans were synthesized in good yields via the one-pot reaction of bis-propargyl alcohols with naphthols. Temperature-dependent photochromism in 1,4-phenylene-linked bispyrans leads to up to 60 nm bathochromic shift between the colored species formed at room temperature and at -20 degrees C. Better fatigue resistance and higher colorability was observed in 1,4-phenylene-linked bis-[2H]-naphtho[1,2-b]pyrans by comparison to the 1,3-phenylene linked bis-[2H]-naphtho[1,2-b]pyrans.  相似文献   

17.
Polyaromatic thiophene compounds are found to occur concomitantly with numerous coal-derived products and shale oils and are suspected mutagens and/or carcinogens. The first synthesis of the two title compounds 9 and 16 has been achieved in five or four steps starting from 8,9-dihydroacenaphtho[1,2-b]benzo[d]thiophene (1) and 7-methoxynaphtho[1,2-b]thiophene (12), respectively. Compound 1 was converted to the cis-diol (11) (via treatment with OsO(4)/pyridine) or to trans-diol (3) [via Prevost reaction (PhCOOAg/I(2)) followed by hydrolysis] in 95-98% yield, respectively. Subsequent dehydration (PTS/benzene) of the diol followed by aromatization of the resulting ketone (5) produced the phenolic compound 6 in 97% yield. Oxidation of the phenol with phenyl iododiacetate followed by hydrolysis of the o-quinone monoketal 7 gave the o-quinone (8) in 86% yield. Stereoselective reduction of 8 with NaBH(4)/EtOH under oxygen afforded trans-10,11-dihydroxy-10,11-dihydroacenaphtho[1,2-b]benzo[d]thi oph ene(9) (orange yellow solid) in 55% yield. Compound 16 was obtained as a colorless solid, through the stereoselective reduction of the o-quinone 15 (with NaBH(4)), which in turn was prepared from 12 following the protocol of functional group transformation of methoxy --> phenol --> o-quinone monoketal --> o-quinone, as used in the previous case. The yields for all the steps are very good. The mutagenicity assay of compound 9 and 16 as well as their parent thiaarenes have been performed. The results showed that 9 may not be the proximate carcinogen of acenaphtho[1,2-b]benzo[d]thiophene, while it is likely that compound 16 is one of the possible proximate carcinogens for naphtho[1,2-b]thiophene.  相似文献   

18.
A series of novel imidazo[1,2-b]isoxazoles 3 and their Mannich bases 4–6 were synthesized via convenient reactions. The reaction of 3-aminoisoxazole 1 with substituted phenacyl bromides 2 in dry ethanol afforded the corresponding 6-methyl-3-aryl imidazo[1,2-b]isoxazoles 3 in good yields.Compounds 3 on treatment with 37% formaline and secondary amines furnished the corresponding novel Mannich bases viz., 6-methyl-3-aryl-2-(morpholine/pyrrolidin-1-yl/piperidin-1-yl)-methyl-imidazo[1,2-b]isoxazoles 4–6.  相似文献   

19.
Reaction of 1,2-hydroxylaminooximes with acetylacetone gives tetrahydroimidazo[1,2-b]isoxazoles. 4-Phenyltetrahydroimidazo[1,2-b]isoxazole in methanolic HCl forms the corresponding 2-acetonyl-2H-imidazole. Both tetrahydroimidazo[1,2-b]isoxazoles and 2-acetonyl-2H-imidazole on heating in aqueous KOH convert into 4-oxo-1,2,3,4-tetrahydropyridines along with 3-acetyl-1-hydroxypyrroles.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 6, pp. 765–771, June, 1990.  相似文献   

20.
The structures of the products of reactions of 1-N-morpholinooxahi-1,2-dihydrothiazolo-[5,4-b]pyridine have been studied by IR, NMR, UV, and mass spectroscopy. Geometric (cis-anti) and rotational (about the CO-N amide bond) isomers of 1-N-morpholinooxalyl-2-propionyi-5-chloro-1,2-dihydrothiazolo-[5,4-b]pyridine oxime have been observed and studied. Treatment of 1-N-morpholinooxalyl-2-propionyl-5-chloro-1,2-dihydrothiazolo[5,4-b]pyridine with ethanolic alkali gave 2-propionyl-5-chlorothiazolo-[5,4-b]pyridine, while treatment with concentrated H2SO4 gave 1,2-dioxo-ethylidene-7-chloroxazolidino[3,2-f]pyrido[2,3-b]1,4-thiazine.For Communication 47 see [1].Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 8, pp. 1133–1138, August, 1993.  相似文献   

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