共查询到20条相似文献,搜索用时 125 毫秒
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青蒿亦称黄花蒿(Artemisia annua L.),为菊科植物,我国民间用于治疗疟疾。据报道,该植物的主要成分为挥发油、烯炔和倍半萜内酯。倍半萜内酯有青蒿素、青蒿甲素、青蒿乙素及青蒿丙素(脱氧青蒿素)。此外,还有青蒿酸、香豆素及黄酮等。我们由山东七、八月所产青蒿提取物中分到青蒿素、青蒿甲素、青蒿乙素、青蒿丙 相似文献
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《有机化学》2015,(5)
以双氢青蒿素为起始原料,经胺化、氧化、烷基化、酯化反应,快速、高效地合成了一系列青蒿砜系列衍生物,目标化合物的结构通过IR、1H NMR、13C NMR和HRMS得到了确证;以四甲基偶氮唑盐比色法(MTT法),研究了该类化合物对人肝癌细胞株SMMC-7721的抗癌活性.初步研究结果表明,该类化合物具有明显地抑制人肝癌细胞增殖、诱导其凋亡的细胞活性,给药72 h,半数抑制浓度IC50最优值为0.06μmol/L.同时采用Annexin/PI流式细胞分析法检测化合物7b对人肝癌细胞SMMC-7721的凋亡情况,结果显示实验组与正常对照组相比人肝癌细胞早期凋亡率和总凋亡率均显著增加.在与青蒿素、双氢青蒿素(DHA)和青蒿砜的对比实验中发现,该类化合物的抗肿瘤活性明显提高,表现出了该类化合物在抗癌药物开发方面具有潜在的应用价值. 相似文献
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Treatment of 2-methyl-7-chloroceramidonine with aqueous ammonia gives 2-methyl-6-amino-7-chloro-ceramidonine, while treatment with sodamide gives 2-methyl-7-chloro-8-aminoceramidonine. 相似文献
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J. Donald Albright Lester A. Mitscher Leon Goldman 《Journal of heterocyclic chemistry》1970,7(3):623-627
Catalytic reduction of apoyohimbine ( 1 ), prepared from yohimbine and thionyl chloride in pyridine, gives methyl yohimbane-16α-carboxylate ( 2 ) after equilibration with methoxide. LAH reduction of 2 or β-yohimbine O-tosylate ( 3 ) gives yohimbane-16α-methanol ( 4a ). LAH reduction of 1 affords yohimbane-16α-carboxaldehyde ( 5 ), yohimb-16-ene-16-methanol ( 6a ) and yohimbane-16β-methanol ( 7a ). Structural assignments 6a and 7a are confirmed by mass spectral measurements. Pmr spectra of 4a, 6a and 7a and their O-acetates 4b, 6b and 7b are discussed. LAH reduction of apo-α-yohimbine ( 8 ) affords alloyohimb-16-ene-16-methanol ( 9 ). Dehydrogenation of 4a with palladium black and maleic acid gives 3,5,4,5,6-tetradehydroyohimbane-16α-methanol ( 10 ) iodide, and 7a gives 3,4,5,6-tetradehydroyohimbane-16β-methanol ( 11 ) iodide and picrate. Properties of 10 and 11 differ from those of melinonine E. 相似文献
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V. A. Kaminskii O. Yu. Slabko M. V. Gomolach 《Chemistry of Heterocyclic Compounds》1990,26(7):772-775
Reaction of 1,5-diketones with 1,2-diamino-4-nitrobenzene gave a mixture of the 6- and 7-nitro derivatives of 4a,9-diaza-1,2,4a,9a-tetrahydrofluorene. Oxidation of the 6-nitro derivatives with MnO2 gives para-quinone imines with elimination of the nitro groups. Oxidation of the 7-nitro derivative and oxidative conjugation of 5-nitro-2,2-pentamethylene-1,2-dihydrobenzimidazole with primary amines in the presence of MnO2 gives nitro ortho-quinone imines.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 7, pp. 927–930, July, 1990. 相似文献
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The Michael addition of adenine (6a), 6-chloropurine (6b) and 2,6-dichloropurine (6c) to methyl -chloroacrylate gives high yields of the corresponding adducts (7a-7c). Hydrolysis and amination of 7a gave the adenyl analogue of Willardiine (2). 相似文献
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The reaction of 2-arylamno-6-methylnicotinonitriles with acetic anhydride or benzoyl chloride gives N-acyl-2-arylamino-6-methylnicotinonitriles. Upon treatment with hydrogen chloride in anhydrous ethanol, these products are converted to 2-substituted 1-aryl-1,4-dihydro-7-methyl-4-oxopyrido[2,3-d]pyrimidines. Heating amides of 2-aryl-amino-6-methylnicotinic acids or 1-aryl-2,7-dimethyl-1,4-dihydro-4-oxopyrido[2,3-d]-pyrimidines at reflux with acetic anhydride in the presence of anhydrous sodium acetate gives 1-aryl-2-acetonyl-7-methyl-1,4-dihydro-4-oxopyrido[2,3-d]pyrimidines.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 1, pp. 114–116, January, 1985. 相似文献
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Conclusions The cyclocondensation of 2,5,6-triamino-4-oxo-3,4-dihydropyrimidine and tetraaminopyrimidine with butylthioacetone and 2-butylthiopropanal gives 7-methylpteridines, while the reaction of these pyrimidine derivatives with 2-phthalimidopropanal, 1,1-dibutoxyacetone, 1,1-dichloroacetone, and 1,1-dibromoacetone gives mixtures of 6- and 7-methylpteridines.Translated from Izvestiya Akademii Nauk SSSR, Seriya Khimicheskaya, No. 2, pp. 452–455, February, 1986. 相似文献
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Curt Wentrup 《Helvetica chimica acta》1972,55(2):565-569
Thermolysis of tetrazolopyrazine ( 1 ) in organic solvents gives pyrazinylnitrene ( 2 ) which undergoes ring contraction to 1-cyanoimidazole ( 3 ). 7-Methyl-5-methylthio-tetrazolo[1,5-c]pyrimidine ( 4 ) likewise gives 1-cyano-2-methylthio-4-methyl-imidazole ( 6 ). The two tetrazoles also undergo ring contraction to 1-cyanoimidazoles by gas chromatography, and 1 gives a low yield of 3 by photolysis. Thermolysis of 1 and 4 in cyclohexane gives aminopyrazine ( 7 ) and 6-amino-4-methyl-2-methylthio-pyrimidine ( 8 ), respectively. Tetrazolo[1,5-a]pyrimidines ( 9 ) give only 2-aminopyrimidines ( 10 ). 1-Cyanoimidazole, formed by thermolysis of 1 in acetic acid, reacts further to give 1-acetylimidazole, which with more acetic acid gives imidazole and acetic anhydride. An earlier report [2] of ring expansion of pyrazinylnitrene in acetic acid is discredited. In protic deuteriated solvents (D3O, CH3OD), tetrazolopyrazine reacts as an enamine, specifically exchanging H? C(6) for deuterium. 相似文献
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On the pathway of the catalytic reduction of 6,7-diphenylpterin The pathway of the hydrogen addition to the pyrazine ring of 6, 7-diphenylpterin ( 1a ) during acid-catalyzed reduction was elucidated. Initial hydrogenation of the 5, 6-double bond produces 6, 7-diphenyl-5, 6-dihydropterin ( 2a ); this then undergoes a [1, 2]-H-rearrangement, which yields the thermodynamically more stable 6, 7-diphenyl-7, 8-dihydropterin ( 3a ). Subsequent reduction of 3a gives 4 . 相似文献
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Schotes C Althaus M Aardoom R Mezzetti A 《Journal of the American Chemical Society》2012,134(2):1331-1343
Hydride abstraction from the β-position of the enolato ligand of the previously reported complex [Ru(3a-H)(PNNP)]PF(6) (5a; 3a-H is the enolate of 2-tert-butoxycarbonylcyclopentanone) with (Ph(3)C)PF(6) gives the dicationic complex [Ru(6a)(PNNP)](2+) (7a) as a single diastereoisomer, which contains the unsaturated β-ketoester 2-tert-butoxycarbonyl-2-cyclopenten-1-one (6a) as a chelating ligand. The methyl analogue 2-methoxycarbonylcyclopentanone (3b) gives [Ru(3b-H)(PNNP)]PF(6) as a mixture of noninterconverting diastereoisomers (ester group of 3b trans to P, 5b; or to N, 5c), which were separated by column chromatography. Hydride abstraction from 5b (or 5c) yields diastereomerically pure [Ru(6b)(PNNP)](2+) (7b or 7c). Complexes 7b and 7c do not interconvert at room temperature in CD(2)Cl(2) and form opposite enantiomers of the Diels-Alder adduct upon reaction with Dane's diene (1 equiv). X-ray studies of 7a, 5b, and 5c give insight into the origin of enantioselection and the sense of asymmetric induction in the previously reported asymmetric Diels-Alder and Ficini cycloaddition reactions with 2,3-disubstituted butadienes and ynamides, respectively. Stoichiometric reactions (substrate coordination, cycloaddition, and product displacement) between [Ru(OEt(2))(2)(PNNP)](2+) (2), 6b (or 6a), and Dane's diene (15, to give estrone derivatives) or N-benzyl-N-(cyclohexylethynyl)-4-methylbenzenesulfonamide (17, to give cyclobutenamides) suggest that product displacement from the catalyst is turnover limiting. 相似文献
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P. M. Kochergin E. V. Aleksandrova V. S. Korsunskii 《Chemistry of Heterocyclic Compounds》2000,36(1):74-76
Treatment of 2-chloro-6-thio-7-methylpurine with aniline, piperidine, or morpholine with heating in DMF gives 2-phenylamino(piperidino or morpholino)-6-thio-7-methylpurine. The scheme for the formation of the side products 2,6-dithio-and 2,6-dipiperidino-7-methylpurine is discussed.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 1, pp. 82–84, January, 2000. 相似文献