• Title/Summary/Keyword: 2-aminopyrimidine

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New Fused Quinoxalines : Synthesis and Reactions of Pyrimidothienoquinoxaline and Oxadizolylthienoquinoxalines

  • Moustafa, Osama S.;Badr, Mahmoud Z.A.;El-Emary, Talaat I.
    • Bulletin of the Korean Chemical Society
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    • v.23 no.4
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    • pp.567-570
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    • 2002
  • Diazotization of 3-amino-2-ethoxycarbonylthieno[2,3-b]quinoxaline 1 gave the diazonium salt 2 which was reacted with SO2 and N-methylaniline to give sulfamoylquinoxaline derivatives 3-5. Imidazothienoquinoxaline 8 was obtained from the reaction of carboxylic acid hydrazide 6 with nitrous acid and followed by boilling the carboazide 7 in dry xylene. Also, compound 6 react with CH(OEt)3 to give aminopyrimidine 9 which was reacted with arylidene malonodinitrile, furfural and/or dimethoxy-tetrahydrofuran to afford compounds 10, 11 and/or 12 respectively. Refluxing of 6 with CS2 gave oxadiazolylthienoquinoxaline 13, reaction of 13 with hyrazine hydrate, CH(OEt)3, nitrous acid, CS2 and a-halocompounds to give 14-19.

Synthesis of N,N-Diaryl-(pyridin-3-yl)pyrimidin-2-amine Derivatives and Their Photochemical Properties

  • El-Deeb, Ibrahim Mustafa;Lee, So-Ha
    • Journal of the Korean Applied Science and Technology
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    • v.25 no.3
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    • pp.291-298
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    • 2008
  • Although the pyrimidine derivatives were obtained in low yields ranging from 8% to 20%, we reported the successful preparation of N,N-diaryl-pyrimidin-2-amine derivatives starting from the corresponding 2-aminopyrimidines (1a-1c), by direct palladium-catalyzed arylation using different arylbromides. The reasons of low yields are thought to be the electronic and steric effects by the neighboring aromatic systems. The absorption spectra and photoluminescent spectra of compounds (3a 3g and 4a-4c) were measured using dichloromethane on the concentration of 25 mM by UV vis spectroscopy and luminescent spectroscopy. Pyrimidine derivatives 4a, 4b, and 4c showed moderate emission maxima at 474 nm, 481 nm, and 367 nm, respectively, while other compounds showed very weak photoluminescence or no photoluminescence at all.

Synthesis of a New 4-(Pyridin-3-yl)pyrimidine Derivatives for Anticancer Activity

  • Jung, Se-Jin;El-Deeb, Ibrahim Mustafa;Lee, So-Ha
    • Journal of the Korean Applied Science and Technology
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    • v.26 no.1
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    • pp.29-37
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    • 2009
  • This study is focused on the synthesis of urea and amide derivatives particularly, since the amide moiety is an essential binding group at the binding site. Urea derivatives 3-7 and 13-14 were obtained by reaction of 2-aminopyrimidines and other amines with diverse isocyanates in pyridine as a solvent under reflux. The urea derivatives were obtained in low yield because of the highly electron deficient nature of the amino group of the 2-aminopyrimidine. Amide derivatives 8-10 were obtained in moderate yields by reaction of compound 1 with aryl chloride derivatives. Also, arylamine 11 was synthesized by Buchwald-Hartwig amination in moderate yields. Most of the compound did not show good activity against A375P melanoma cells, compared with Sorafenib as control compound.

Reaction of Nitrous Acid on 5-Aminopyrimidines [III] Sandmeyer Reaction of Diazotizated 5-Amino-6-Methyluracil (Aminopyrimidine 유도체에 대한 아질산의 작용 [III] Diazotizated 5-Amino-6-Methyluracil에 대한 Sandmeyer 반응)

  • Chang, Sae-Hee;Hahn, Bo-Sup;Kim, In-Kyu;Oh, Sea-Hwa
    • Journal of the Korean Chemical Society
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    • v.10 no.2
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    • pp.51-53
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    • 1966
  • A new conventional method for the preparation of 5-iodo, chloro-, and bromo-6-methyluracil by Sandmeyer reaction was described. According to this procedure, 5-halo-6-methyluracils have been prepared in high yields (up to 70%) without any difficulties to obtain highly pure products. No appreciable competing reaction was observed.

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BMI-1026 treatment can induce SAHF formation by activation of Erk1/2

  • Seo, Hyun-Joo;Park, Hye-Jeong;Choi, Hyung-Su;Hwang, So-Yoon;Park, Jeong-Soo;Seong, Yeon-Sun
    • BMB Reports
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    • v.41 no.7
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    • pp.523-528
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    • 2008
  • BMI-1026 is a synthetic aminopyrimidine compound that targets cyclin dependent kinases (cdks) and was initially designed as a potential anticancer drug. Even though it has been well documented that BMI-1026 is a potent cdk inhibitor, little is known about the cellular effects of this compound. In this study, we examined the effects of BMI-1026 treatment on inducing premature senescence and then evaluated the biochemical features of BMI-1026-induced premature senescence. From these experiments we determined that BMI-1026 treatment produced several biochemical features of premature senescence and also stimulated expression of mitogen activated protein kinase (MAPK) family proteins. BMI-1026 treatment caused nuclear translocation of activated Erk1/2 and the formation of senescence associated heterochromatin foci in 5 days. The heterochromatin foci formation was perturbed by inhibition of Erk1/2 activation.