共查询到19条相似文献,搜索用时 621 毫秒
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以4-氯-6,7-二甲氧基喹唑啉、8-溴辛酸乙酯及溴代正丁烷等为原料,根据喹唑啉类化合物药效结构关系,对N-(3-氯-4-烷氧苯基)喹唑啉-4-胺类化合物(ARRY-334543)进行了结构修饰,合成了具有抗肿瘤细胞活性的酪氨酸激酶抑制剂。采用NMR和MS对化合物的结构进行了表征,并对其进行了抗肿瘤细胞活性测试。得到的化合物IX a ~ b均对MCF-7、BGC-823、A549、DU145和H1975细胞有一定的抗肿瘤活性,活性最好的是化合物IX a,其半数抑制浓度(GI50)为0.37μmol/L。 相似文献
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报道一种9-氯-6,7-二甲氧基-2,3-二氢-1H-环戊二烯并[b]喹啉的简便制备方法。以2-氨基-4,5-二甲氧基苯甲酸和环戊酮为原料,在三氯氧磷作用下"一锅法"合成目标化合物9-氯-6,7-二甲氧基-2,3-二氢-1H-环戊二烯并[b]喹啉。产物结构经~1H NMR和ESI-MS确证。最佳反应条件为:环戊酮用量为1.5当量,120℃反应12 h,产物收率76.4%。按照最佳反应条件对于底物进行拓展,2-氨基-4,5-二甲氧基苯甲酸和环己酮反应得到9-氯-6,7-二甲氧基-1,2,3,4-四氢吖啶,收率64.2%。 相似文献
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研究了以3-氯-5-甲氧基-2,6-二硝基吡啶为原料,通过甲氧化、硝化、氨化合成3-甲氧基-5,6-二氨基-2-硝基吡啶,该化合物的结构通过IR,1H NMR,MS和元素分析进行了表征,确认为目标化合物。分析了3-甲氧基-5-氯-2,6-二硝基吡啶的氯基和硝基的反应活性。 相似文献
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以N′-(5-(3-氯丙氧基))-2-氰基-4-甲氧苯基-N,N-二甲基甲脒为原料,经过成环、醚化,合成了4个4-(3′-氯苯氨基)-6-甲氧基喹唑啉类化合物:N-(3′-氯苯基)-6-甲氧基-7-(3-(4-硝基苯氧基)丙氧基)喹唑啉-4-胺、N-(3′-氯苯基)-6-甲氧基-7-(3-(3-硝基苯氧基)丙氧基)喹唑啉-4-胺、4-(3-(4-(3′-氯苯胺基)-6-甲氧基喹唑啉-7-基氧基)丙氧基)-3-甲氧基苯甲醛、3-(3-(4-(3′-氯苯胺基)-6-甲氧基喹唑啉-7-基氧基)丙氧基)-4-甲氧基苯甲醛,收率分别为51.3%、60.3%、85.4%、79.4%。产物的结构经红外光谱、核磁共振氢谱、核磁共振碳谱、质谱和元素分析表征。采用MTT法进行化合物抑制Bcap-37细胞的体外活性测试,结果表明:合成的化合物具有不同程度的抑制Bcap-37细胞的活性, 其中化合物Ιa在10 μmol?L-1浓度下对Bcap-37细胞的抑制率为83.4%。 相似文献
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以N'-[5-(3-氯丙氧基)]-2-氰基-4-甲氧苯基-N,N-二甲基甲脒为原料,经过成环、醚化,合成了4个4-(3'-氯苯氨基)-6-甲氧基喹唑啉类化合物(Ⅰa~Ⅰd):N-(3'-氯苯基)-6-甲氧基-7-[3-(4-硝基苯氧基)丙氧基]喹唑啉-4-胺(Ⅰa)、N-(3'-氯苯基)-6-甲氧基-7-[3-(3-硝基苯氧基)丙氧基]喹唑啉-4-胺(Ⅰb)、4-{3-[4-(3'-氯苯胺基)-6-甲氧基喹唑啉-7-基氧基]丙氧基}-3-甲氧基苯甲醛(Ⅰc)、3-{3-[4-(3'-氯苯胺基)-6-甲氧基喹唑啉-7-基氧基]丙氧基}-4-甲氧基苯甲醛(Ⅰd),收率分别为51.3%、60.3%、85.4%、79.4%。产物的结构经IR、1HNMR、13CNMR、MS和元素分析表征。采用MTT法进行化合物抑制Bcap-37细胞的体外活性测试,结果表明,合成的化合物具有不同程度抑制Bcap-37细胞的活性,其中化合物Ⅰa在10μmol/L浓度下对Bcap-37细胞的抑制率为83.4%。 相似文献
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2-氯-6,7-二氢喹啉培(5H)-酮是四氢喹啉是一个重要的含氮杂环化合物。文章以2-氯-5,6,7,8-四氢喹啉为原料,经氧化、酯化、水解反应后得到2.氯-5,6,7,8-四氢喹啉-8-醇,再经Anelli氧化后得到总收率为57,8%的目标产物。所得化合物的结构均经核磁和质谱确证。 相似文献
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Enantiomerically enriched forms of (Z)-6-cis-9,10-epoxymonoenes and (Z)-9-cis-6,7-epoxymonoenes of chain lengths C17–20 were synthesized by Sharpless asymmetric epoxidation of allylic alcohol intermediates, followed by tosylation or halogenation and chain extension. The resulting monounsaturated epoxides were field tested as sex attractants for lepidopteran species.Euchlaena madusaria Walker males were attracted to blends of the enantiomers of (Z)-6- cis- 9,10-epoxynonadecene 6Z-cis-9,10-epoxy-19:H; IUPAC name [2,3(Z)]-2-pentyl-3-(2-dodecenyI)oxirane in combination with 6Z,9Z-19: H. The response was antagonized by 9Z-cis-6,7-epoxy-19: H. 6Z,9Z-19: H was tentatively identified in pheromone gland extracts.Xanthotype sospeta Drury male moths were attracted to lures containing 6Z-9S,10R-epoxy-19: H; the response was antagonized by the opposite enantiomer.Pal-this angulalis Hübner males were attracted to 9Z-6S,7R-epoxy-19:H; the opposite enantiomer was antagonistic. 6Z,9Z-19:H and 9Z-cis-6,7-epoxy-19:H and 9Z-cis-6,7-epoxy-19:H were tentatively identified in pheromone gland extracts fromAnacamptodes humaria Guenée females. In field trails, 9Z-6R,7S-epoxy-19:H proved to be the attractive enantiomer, and the response was potentiated by 6Z,9Z-19:H. Mechanisms by which unique chemical communication channels are maintained by each species are discussed.1 Issued as NRCC #32455. 相似文献
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采用胡椒醛为原料,经硝化、还原得到邻氨基胡椒醛,再在乙醇钠的催化下,与2-丁酮酸发生Friedland缩合反应,合成了新化合物3-甲基-6,7-亚甲二氧基-2-喹啉酸。通过^1H NMR、IR和元素分析表征了新化合物的结构。 相似文献
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Kenneth F. Haynes Kenneth V. Yeargan Jocelyn G. Millar Bonnie B. Chastain 《Journal of chemical ecology》1996,22(1):75-89
The bolas spider,Mastophora hutchinsoni, attracts adult males of four species of nocturnally active Lepidoptera through aggressive chemical mimicry of those species' sex pheromones. Here we report the identification of the sex pheromone of one prey species, the smoky tetanolita (Tetanolita mynesalis). In sex pheromone gland extracts, only two peaks stimulated an electrophysiological response as measured by a coupled gas chromatography-electroantennographic detection analysis. These two peaks had retention times identical to (3Z,6Z,9Z)-heneicosatriene (3Z,6Z,9Z-21:H) and (3Z,9Z)-cis-6,7-epoxy-heneicosadiene (3Z,9Z-cis-6,7-epoxy-21:H), respectively, and mass spectra identical to these two compounds. It was determined that 0.23±0.16 and 0.56±0.26 ng of 3Z,6Z,9Z-21:H and 3Z,9Z-cis-6,7-epoxy-21:H, respectively, were present in pheromone gland extracts from individual females. A 1:1 blend of 3Z,6Z,9Z-21:H and 3Z,9Z-6S,7R-epoxy-21:H was an effective attractant for adult males from feral populations. Blend ratios of these two components from 2:1 to 1:2 were equally effective as attractants. Greater deviation from the optimal blends resulted in diminished trap catches. The enantiomer 3Z,9Z-6R,7S-epoxy-21:H not only was not effective in attracting males, its presence in the effective blend shut down trap catches. These results indicate that the pheromone blend consists of 3Z,6Z,9Z-21:H and 3Z,9Z-6S,7R-epoxy-21:H. This is the first report of a hydrocarbon/epoxide pheromone for a prey species of this bolas spider. Sex attractants or pheromones for the other three prey species are composed of aldehydes or acetates. 相似文献
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Microbial transformation studies conducted on isopimpinellin (1) by the fungus Glomerella cingulata have revealed that 1 was metabolized to give the corresponding reduced acid, 5,8-dimethoxy-6,7-furano-hydrocoumaric acid (2). The structure of metabolite 2 was elucidated by high-resolution mass spectrometry (HR-MS), extensive NMR techniques, including (1)H NMR, (13)C NMR, (1)H-(1)H correlation spectroscopy (COSY), heteronuclear multiple quantum coherence (HMQC) and heteonuclear multiple bond coherence (HMBC). The biotransformed product 2 showed weak a in vitro β-secretase (BACE1) inhibitory effect. 相似文献