• Title/Summary/Keyword: 2-Aryl-2

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Asymmetric synthesis of (2S, 3R, 4E) 5-Aryl-4-pentene-1,3-diol-2-aminoueras

  • Im, C.U.;Kim, Y.H.;Jyung, M.L.;Lim, C.B.
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.237.1-237.1
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    • 2003
  • (2S 3R. 4E) 5-Aryl-4-pentene-1,3-diol-2-aminoueras had been synthesized for their cytotoxic activity. Pinene was oxidized with KMnO4 to give 2-hydroxy-3-pinanone. which treated with ethyl glycinate to yield iminoglycinate and then reacted with aldehyde derivatives and titanium enolate to afford 3-hydroxy aldol compounds. (omitted)

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Synthesis and Fungitoxicity of Some Pyrimidine Derivatives

  • Ouf, Salama A.;Sherif, Sherif M.
    • Archives of Pharmacal Research
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    • v.16 no.1
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    • pp.62-67
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    • 1993
  • A series of 12 pyrimidine derivatives were prepared and tested in vitro against growth, sporulation and nucleic acids of Fusarium oxysporum f. sp. lycopersici and Helminthosporium oryzae. Intorduction of thiazole ring together with two aryl groups to 2-aminopyrimidine induced drastic toxicity for both fungi. Pyrimidine derivatives with aryl groups were less toxic. Nitro groups were found to enhance the toxicity of the pyrimidine derivatives especially when substituted in ortho-position of the aryl groups. Inhibition of nudeic acids synthesis of both fungi was attributed mainly to the presence of thiazole ring.

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Preparation, Characterization and First Application of Alumina Supported Polyphosphoric Acid (PPA/Al2O3) as a Reusable Catalyst for the Synthesis of 14-Aryl-14H-dibenzo[a, j]xanthenes

  • Norouzi, Haniyeh;Davoodnia, Abolghasem;Bakavoli, Mehdi;Zeinali-Dastmalbaf, Mohsen;Tavakoli-Hoseini, Niloofar;Ebrahimi, Mahmoud
    • Bulletin of the Korean Chemical Society
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    • v.32 no.7
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    • pp.2311-2315
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    • 2011
  • Alumina supported polyphosphoric acid (PPA/$Al_2O_3$) was successfully prepared by impregnation of alumina support by polyphosphoric acid and characterized using FT-IR spectroscopy, the $N_2$ adsorption/desorption analysis (BET), thermal analysis (TG/DTG), and X-ray diffraction (XRD) techniques. The catalytic behavior of this new solid acid supported heterogeneous catalyst was checked in the synthesis of 14-aryl-14H-dibenzo[a, j]xanthenes by cyclocondensation reaction of ${\beta}$-naphthol and aryl aldehydes under solvent-free conditions. The results showed that the novel catalyst has high activity and the desired products were obtained in very short reaction times with high yields. Moreover, the catalyst can be easily recovered by filtration and reused at least three times with only slight reduction in its catalytic activity.

1,2,4-Triazinylmethylphenyl Glucoside as Novel C-Aryl Glucoside SGLT2 Inhibitors

  • Kang, Suk-Youn;Kim, Min-Ju;Lee, Jin-Hwa
    • Bulletin of the Korean Chemical Society
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    • v.32 no.spc8
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    • pp.2938-2940
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    • 2011
  • Novel C-aryl glucoside SGLT2 inhibitors containing triazine motif were designed and synthesized for biological evaluation. Among the compounds assayed, triazine containing methoxy moiety 18 demonstrated the best in vitro inhibitory activity against hSGLT2 in this series to date ($IC_{50}$ = 24.9 nM).

Synthesis of 2-Arylbenzothiazoles Catalyzed by Biomimetic Catalyst, β-Cyclodextrin

  • Londhe, Balaji S.;Pratap, Umesh R.;Mali, Jyotirling R.;Mane, Ramrao A.
    • Bulletin of the Korean Chemical Society
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    • v.31 no.8
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    • pp.2329-2332
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    • 2010
  • Cyclocondensation of 2-aminothiophenol and aryl/heteryl aldehydes has been carried using biomimetic catalyst, $\beta$-Cyclodextrin in water and obtained 2-aryl/heteryl benzothiazoles with better to excellent yields. This biomimetic catalyzed route is simple, economic, and environmentally benign.

Synthesis of 2,7-Methano-aza[10]annulene Derivatives

  • 김충섭
    • Bulletin of the Korean Chemical Society
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    • v.17 no.5
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    • pp.437-442
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    • 1996
  • Electrocyclic ring-closure of 6-vinylcyclohepta-1,3,5-isocyanate has been carried out in the presence of triphenylphosphine to examine a catalyzing effect of the triphenylphosphine. The preparation of 10-(1-carboalkoxyalkyl)-2,7-methanoaza[10]annulenes by the electrocyclic ring-closure of ketenimine intermediates, which are formed by the reaction of triphenylalkylidenephosphorane and 6-vinylcyclo-hepta-1,3,5-isocyanate, is described. 10-Alkyl-2,7-methanoaza[10]annulenes were prepared by basic hydrolysis of the carboalkoxyaza[10]annulenes and decarboxylation of the acid intermediates. In the same manner, 10-(N-alkyl(or aryl))-2,7-methanoaza[10]annulenes were prepared from the reaction of the isocyanate and N-alkyl(or aryl)iminotriphenylphosphorane via electrocylic ring-closure of carbodiimide intermediate.

Aminolysis of Aryl Thiol-2-furoates and Thiol-2-thiophenates in Acetonitrile

  • 오혁근;이준용;이익춘
    • Bulletin of the Korean Chemical Society
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    • v.19 no.11
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    • pp.1198-1202
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    • 1998
  • Aminolysis of aryl thiol-2-furoates and thiol-2-thiophenates with benzylainines are investigated in acetonitrile at 50.0 ℃. Relatively large selectivity parameters, ρx(βx), ρz(βx) and ρxz (> 0) together with the valid reactivity-selectivity principle are consistent with a stepwise acyl transfer mechanism with rate-limiting expulsion of the leaving group, thiophenolate anion, from the tetrahedral intermediate, T±. The first-order kinetics with respect to the benzylamine concentration and the relatively large secondary kinetic isotope effect involving deuterated benzylamine nucleophiles suggest a four-center type transition state in which concurrent leaving group departure and proton transfer are involved.

Antifungal activity of N-[1-(benzotriazol-1-yl)aryl]arylamine derivatives and quntitative structure-activity relationships(QSAR) (N-[1-(benzotriazol-1-yl)aryl]arylamine 유도체의 항균성과 정량적 구조활성 관계(QSAR))

  • Sung, Nack-Do;Kim, Kyoung-Hoon;Choi, Woo-Young;Kim, Hong-Ki
    • Applied Biological Chemistry
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    • v.35 no.1
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    • pp.14-22
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    • 1992
  • A series of new N-[1-(benzotriazol-1-yl)aryl]arylamine derivatives were synthesized and their antifungal activities $(pI_{50})$ in vitro against Pyricularia oryzae, Fusarium oxysporum f. sp. sesami, Valsa ceratosperma and Botrytis cinerea were dertermined by the agar medium dilution method. From the results of the quantitative structure-activity relationships $(QSAR_S)$ analysis, $hydrophobicity({\pi})$, $electronic({\Sigma\sigma})$ and molar $refractivity({\Sigma}M_R)$ parameter of X & Y-substituents on the phenyl group were also shown to be important factor in determining the variation in the antifungal activity. 4-Bromo group substituents (1d & 2b) were the most effective compounds and the $half-life(T_{1/2})$ on the hydrolysis of X(1) at netural pH was about 1.5 day. Molecular orbital(MO) functions of substrate compound, linear free energy relationships$(LFER_S)$ on the antifungal reactivity arid the results of molecular design were also discussed.

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