• Title/Summary/Keyword: derivative synthesis

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Investigation of the Reaction of 6-Amino-3-methyl-4-oxo-3, 4-dihydro-2-pyrimidinylhydrazine

  • Moustafa, M.A.;Gineinah, M.M.;Bayomi, S.M.;Ismaiel, A.M.
    • Archives of Pharmacal Research
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    • v.13 no.4
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    • pp.347-350
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    • 1990
  • The hydrazine derivative 2 has been utilized for the synthesis of three different fused 1, 2, 4-triazolo [4, 3-a] pyrimidine derivatives 4, 5, &6 and a tetrazolo [1, 5-a] pyrimidine derivative 7. Reaction of 2 with the chalcone analogue 2-thenylidene-2'-acetothienone, gave the pyrazoline derivative 8.

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Heterocyclic Synthesis with Nitriles: New Routes for Synthesis of Pyridazines, Pyridines and their Fused Derivtives

  • Negm, Abdalla-M.;Abdelrazek, Fathy-M.;Elnagdi, Mohamed-H.;Shaaban, Lina-H.
    • Archives of Pharmacal Research
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    • v.17 no.6
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    • pp.411-414
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    • 1994
  • Phenylazocyanothioacetamide 1 reacts with malononitrile to afford the pyridinethione 4 which reacts with phenacylbromide to yield the pyridine-S-phenacyl derivative 6, 1 reacts with ethyl cyanoacetate to yield the pyridazine derivative, 8, and with phenacyl bromide to afford the N-phenacyl derivative 11, instead of the thiazole 10. Compound 11 afforded the pyrazolopyridine 13 on reaction with malononitrile while 10 was obtained on coupling of the thiazole 14 with diazotised aniline. Compound 10 reacts with malononitrile to afford the thizaolyl pyridazine 15. Compound 1 reacts with malononitrile dimer to afford the pyriodopyridazine derivative 17a. 1 reacts also with active methylene heterocycies to afford the pyrazolo and thiazolo-fused phridazines 20 and 23 respectively.

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A Novel Synthesis of Heterocyclic Compounds Containing Coumarin Moiety of Potential Antimicrobial Activity

  • El-Fattah, M. E. Abd
    • Archives of Pharmacal Research
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    • v.21 no.6
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    • pp.723-728
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    • 1998
  • The chemical behaviours of 4-methyl-2-oxo-2H-benzopyran-7-yl oxoacetyl hydrazine (2) towards some different reagents such as anhydride compounds, aromatic aldehydes, carb on disulphide, and nitrous acid yielded the corresponding pathalazine derivatives (3, 4, 5), hydrazone derivative (6), 1,3,4-oxadiazole derivative (7, 8, 9) and acid azide (10) respectively. Treatmen of 10 with absolute alcohols, amines and ethyl amino acid ester gave the corresponding carbamate derivative (11), substituted urea derivative (12) and ethyl substituted alkyl acetate (13) respectively. The biological activity of some synthesized compounds was evaluated.

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Synthesis and Electrorheological Effect of the Suspensions Composed of Nano Sized Hollow Polyaniline Derivatives

  • Choi Ung-Su
    • KSTLE International Journal
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    • v.7 no.1
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    • pp.18-21
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    • 2006
  • The electrorheology of hollow PANI derivative suspensions in silicone oil was investigated by varying the electric fields and shear rates, respectively. The hollow PANI derivative susepnsions showed a typical electrorheological (ER) response caused by the polarizability of an amide polar group and shear yield stress due to the formation of chains upon application of an electric field. The shear stress for the hollow PANI succinate suspension exhibited an electric field power of 0.67. On the basis of the experimental results, the newly synthesized hollow PANI derivative suspensions were found to be an anhydrous ER fluid.

Concise Synthetic Approaches to Naturally Occurring β-Hydroxypyranochalcones: First Total Synthesis of Purpurenone, Its Derivative, and Praecansone B

  • Wang, Xue;Lee, Yong-Rok;Kim, Sung-Hong
    • Bulletin of the Korean Chemical Society
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    • v.33 no.8
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    • pp.2647-2650
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    • 2012
  • The total synthesis of biologically interesting ${\beta}$-hydroxypyranochalcones, purpurenone (1), its derivative 2, praecansone B (3), and pongapinone A (4) has been accomplished starting from commercially available 2,4-dihydroxyacetophenone or 6-methoxy-2,4-dihydroxyacetophenone in 3 steps by a convergent strategy through benzopyran formations, O-methylations, and coupling reactions.

Design and Synthesis of Carbo Analog of Oxetanocin Bisphosphate Derivative as $P2Y_1$ Receptor Antagonist ($P2Y_1$ 수용체 길항제로서의 옥세타노신 카보 유도체의 설계 및 합성)

  • 김혜옥
    • YAKHAK HOEJI
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    • v.43 no.3
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    • pp.328-333
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    • 1999
  • In order to develop selective and competitive and competitive antagonist at the $P2Y_1$ receptor a carbocyclic oxetanocin bisphosphate derivative (7) was synthesized as a bioisostere of the lead, MRS 2179. The synthesis was started from ketene diethylacetal (1) and completed in 6 steps.

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Synthesis of Pyrrolo[2,3-c]acridines

  • Munawar Ali Munawar;Paul W. Groundwater
    • Bulletin of the Korean Chemical Society
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    • v.20 no.4
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    • pp.456-458
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    • 1999
  • The synthesis of 6-amino-3-benzylpyrrolo[2,3-c]acridine (9) and its 8,9-dimethoxy derivative (10) from N-benzyl-4,5,6,7-tetrahydroindol-4-one and anthranilonitriles, via imine formation followed by cyclization and aromatisation, is described.

Attempted Synthesis of Carboxin Derivative through Ring Expansion Reaction on Solid Phase (고체상에서 환팽창 반응에 의한 카르복신 유도체의 합성시도)

  • Hahn, Hoh-Gyu;Bae, Su-Yeal;Nam, Kee-Dal
    • The Korean Journal of Pesticide Science
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    • v.9 no.3
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    • pp.185-190
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    • 2005
  • Solid phase synthesis of 16, which is a derivative of the first systemic fungicide, carboxin 1 was described. Reaction of 1,3-oxathiolane derivative with solid resin of 4-hydroxy-3-nitrobenzophenone 6 gave 9 in 82% yield. Oxidation of sulfur in the solid 1,3-oxathiolane 9 by MCPBA followed by a ring expansion reaction under the acid catalyst afforded the corresponding dihydro-1,4-oxathiin derivative 12. Treatment of the solid 1,3-oxathiolane 9 with p-methoxyaniline resulted in 1,3-oxathiolane 14, 1,3-oxathiolane sulfoxide 15, dihydro-1,4-oxathiin 16, and acetoacetanilide derivative 17 in 41%, 35%, 14%, 10% yields, respectively.

Synthesis of Ketoconazole Derivatives

  • Ryu, Jae-Chun;Lee, Kwang-Jae;Lee, Sang-Hee
    • Bulletin of the Korean Chemical Society
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    • v.24 no.4
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    • pp.460-466
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    • 2003
  • For the drug master file (DMF) of ketoconazole, four impurities (1-4) contained in ketoconazole were synthesized. During the synthesis of 2, a new synthetic method of 1,4-dihydropyrazine was established. To oxidize the aminoalcohol (2j) to the aminal (2j-1), the standard Swern oxidation condition was modified to mask the nucleophilicity of the amino group temporarily using one equivalent of acetic acid. Derivative 3 was synthesized via regioselective bromination at the 2 position of the 4-aminophenol derivative (3a) using $Br_2$ in the presence of p-TsOH. The etherification of aryl bromide with the phenol derivative (1f) was accomplished by a modification of the general Cu-mediated reaction condition using excess 1f itself as a solvent at elevated temperature (190 ℃).