• Title/Summary/Keyword: Hydrazine Hydrate

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Some Nucleophilic Substitutions in 2,4- and 2,4,8-Trichloro- pyrido [3,2-d] pyrimidines

  • Boyomi, Said M.;Ismaiel, Abdel-Kader M.;Eisa, Hassan M.;El-Kerdawy, Mohamed M.
    • Archives of Pharmacal Research
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    • v.12 no.1
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    • pp.8-11
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    • 1989
  • Reaction of 6-(acetoxymethyl) -2,4-dichloropyrido [3,2-d] pyrimidine (I) with some nucleophiles was investigated. When I reacted with sodium azide afforded 2,4-diazido derivative (II). Treatment of II with sodium hydroxide underwent cyclization of the 2-azido group to tetrazolo, replacement of 4-azido group by hydroxide ion, and hydrolysis of 6-ace-foxy moiety to hydroxy methyl derivative (III). While, reaction of I with hydrazine hydrate resulted in the formation of 2,4 dihydrozino-6-hydroxymethyl derivative (lV).

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Reactions with Activated Nitriles : A new route for the synthesis of new pyridine and pyrazolopyridine derivatives

  • Attaby, Fawzy-A.;Eldin, Sanaa-M.
    • Archives of Pharmacal Research
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    • v.13 no.3
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    • pp.274-277
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    • 1990
  • It has been found that $\alpha, \beta$-unsaturated nitrile derivatives 1-3 reached with S- methylisothiourea to give the prpone derivatives 4-6 respectively. Cyclisation of 4-6 using ethanolic hydrochloric acid afforded the pyridine derivatives 7-9 in good yields. On the other hand, the reactions of hydrazine hydrate and of phenylhydrazine with each of 7-9 gave the corresponding pyrazolopyridine derivatives 10-15. The structures of the newly synthesised derivatives were assigned on the basis of elemental analyses, IR and $^1H$-NMR spectral data studies.

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Synthesis and Biological Investigations of New Thiazolidinone and Oxadiazoline Coumarin Derivatives

  • Abd Elhafez, Omaima Mohamed;El Khrisy, Ezz El Din Ahmed Mohamed;Badria, Farid;Fathy, Alaa El Din Mohamed
    • Archives of Pharmacal Research
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    • v.26 no.9
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    • pp.686-696
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    • 2003
  • Ethyl (coumarin-4-oxy)acetate 1 was prepared through the reaction of 4-hydroxycoumarin with ethyl bromoacetate. Compound 1 was allowed to react with hydrazine hydrate to produce coumarin-4-oxyacetic hydrazide 2. The synthesis of N-(arylidene and alkylidene)-coumarin-4-oxyacetic hydrazones 3-20 was performed. The preparation of 2-substituted-3-[(coumarin-4-oxy) acetamido]thiazolidinones 21-26 and 2-[(coumarin-4-oxy )methyl]-4-acetyl-5-substituted-$\Delta^2$-1,3,4-oxadiazolines 27-33 was performed by the reaction of the hydrazones 3, 4, 7, 9, 12, 14 with mercaptoacetic acid and the hydrazones 3, 4, 5, 7, 12, 15, 16 with acetic anhydride, respectively. The antiviral activities, cytotoxicities and structure-activity relationship (SAR) towards different microorganisms of the prepared compounds were studied.

Synthesis of some pyridinethione derivatives and their biological activity

  • Miky, Jehane A.A.;Zahkoug, Samir A.M.
    • Natural Product Sciences
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    • v.3 no.2
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    • pp.89-99
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    • 1997
  • Aminolysis, hydrazinolysis and alkylation of 4-methoxy and 4,9-dimethoxy-6-cyano-7-thione-5-methyl-7H furo [3,2-g] [1] benzopyridine (1 a-b) yielded 7N-substituted furobenzopyridine derivatives (2 a-e or the possible isomers 3 a-e and 4 a-b), (5 a,b and 6 a,b) and the ester (8 a,b). Hydrolysis of (la) with acetic acid gave the corresponding pyridone derivatives (7). Furobenzopyridinyl-7-thioacetyl hydrazide (9 a,b) have been prepared via alkylation of furobenzopyridine thione (1 a-b) with ethyl chloroacetate followed by condensation with hydrazine hydrate. Schiff base (11) was prepared by reacting (9a) with p. N,N-dimethyl aminobenzaldehyde in boiling ethanol. Treatment of (8a) with anthranilic acid gave the corresponding 7-substituted-4H-3,1-benzoxazine-4-one (10). We found that compound (11) increased bleeding, coagulating time, the total count of white blood cells, blood glucose level (cause hyperglycemia), enzymes (GOT, GPT) activities, concentration of urea and creatinine. On the other hand it decreased red blood cells number, haemoglobin content and haematocrite value.

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Activated Nitrites in Heterocyclic Synthesis: Syntheses of Thiazole, Pyrazole and 4H-l,4-Benzothiazine Derivatives

  • El-Taweel, Fathy Mohamed Abdel-Aziz;Hadi-Mashaly, Mohamed-Abdel;Ali-Elagamey, Abdel-Ghani
    • Archives of Pharmacal Research
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    • v.13 no.3
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    • pp.261-264
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    • 1990
  • 4-Arylazo-3-phenyl-5-aminopyrazoles (5a, b) and substituted hydroxythiazoles 8a, b were synthesized from the reaction of 4a, b with hydrazine hydrate and mercaptoacetic acid respectively. Compounds 5a, b and 8a, b were also obtained from coupling of 2a, b with 6 and 7, respectively. 4H-1, 4-Benzothiazine 11 was prepared from 1 and 10. The resaction of the diazonium salts 2a-c with diethyl 3-amino-2-cyanopenet-2-en-1, 5-dicarboxylate 12 was also reported.

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One Pot Four-Component Synthesis of Novel Substituted 2-Phenyl-4(3H) Quinazolinones Using Recyclable Nanocrystalline CuMnO3 Catalyst

  • Borhade, A.V.;Tope, D.R.;Gare, G D.;Dabhade, G.B.
    • Journal of the Korean Chemical Society
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    • v.61 no.4
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    • pp.157-162
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    • 2017
  • In the present study, nanocrystalline mixed metal oxide, $CuMnO_3$ catalyst have been synthesized by mechanochemical method with green chemistry approach. The synthesized catalyst was characterized by analytical techniques including FTIR, XRD, SEM, TEM and BET surface area. The synthesized catalyst shows high surface area is $121.06m^2/g$ with particle size 18 nm. The one pot four component synthesis of substituted 2-phenyl-4(3H) quinazolinone from the reaction of anthranilic acid, benzoyl chloride, hydrazine hydrate and substituted benzaldehyde in presence of $CuMnO_3$ nanocatalyst has been carried out. It affords the corresponding products with high yield (76-95%) in very short reaction time. All the obtained products were characterized with $^1HNMR$, $^{13}CNMR$, FTIR and EIMS.

Synthesis of [1,2,4]-Triazole Derivatives Containing Benzimidazole and Biological Activities (Benzimidazole을 함유한 [1,2,4]-Triazole 유도체의 합성 및 생물학적 활성)

  • Lee, So-Ha;Jeon, Jae-Ho;Lim, Hye-Won;Pae, Ae-Nim
    • Journal of the Korean Applied Science and Technology
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    • v.23 no.4
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    • pp.355-361
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    • 2006
  • [1,2,4]-Triazole derivatives were synthesized by 5 steps. Benzimidazole was refluxed with ethyl chloroacetate to give 1H-benzimidazole-acetic acid ethyl ester (1) over 52% yield. Ester (1) was refluxed with hydrazine hydrate in the presence of ethanol to afford 1H-benzimidazole-1-acetic acid, hydrazide (2). 5-Benzoimidazol-1-ylmethyl-4H-[1,2,4]triazole-3-thiol (4) was made via coupling of compound (2) with methyl isothiocyanate, followed by cyclization of 1H-benzimidazole-1-acetic acid, 2-[(methylamino) thioxomethyl]hydrazide (3) on reflux, and finally the target compounds (6a-6v) were synthesized by general substitution reaction. Compounds (6a-6v) were screened for T-type calcium channel blocker using the fluorescence assay by FDSS6000. All compounds (6a-6v) did not show better activities than control compound, mibefradil.

Reduced Graphene Oxide Field-Effect Transistor for Temperature and Infrared Sensing

  • Trung, Tran Quang;Tien, Nguyen Thanh;Kim, Do-Il;Lee, Nae-Eung
    • Proceedings of the Korean Vacuum Society Conference
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    • 2012.02a
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    • pp.552-552
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    • 2012
  • We fabricated reduced graphene oxide field-effect transistor (RGO-FET) on glass for highly sensitive temperature and IR detection. The device has the channels of RGO responsive to physical stimuli such as temperature and IR. The RGO sensing layers are fabricated from exfoliated graphene oxide sheets that are deposited to form a thin continuous network by electrostatic assembly. These graphene oxide networks are reduced toward reduce graphene oxide by exposure to a hydrazine hydrate vapor. To improve performance and eliminate interferences from oxygen and water vapor absorption to electrical properties of RGO-FET, the sensor devices were encapsulated by the tetratetracontane layer after annealing treatment. The device with encapsulation layer showed lower hysteresis, improved stability, and better repeatability. The temperature response of RGO-FET is examined by measuring changing the temperature, the device exhibited the high sensitivity and repeatability even with the temperature interval of 1 K. We also demonstrated that our devices have capability of IR sensing.

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Synthesis of Novel 6,7,8,9-Tetrahydro-5H-5-hydroxyphenyl-2-benzylidine-3-substituted Hydrazino Thiazolo (2,3-b) Quinazoline as Potent Antinociceptive and Anti-inflammatory Agents

  • Selvam, T. Panneer;Kumar, P. Vijayaraj
    • Bulletin of the Korean Chemical Society
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    • v.31 no.11
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    • pp.3265-3271
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    • 2010
  • A series of 6,7,8,9-tetrahydro-5H-5-hydroxyphenyl-2-benzylidine-3-substituted hydrazino thiazolo (2,3-b) quinazolines have been synthesized to meet the structural requirements essential for anti-inflammatory and antinociceptive properties. The synthesized series of heterocycles, 6,7,8,9-tetrahydro-5H-5-hydroxyphenyl-2-benzylidine-3-substituted hydrazino thiazolo (2,3-b) quinazoline by the reaction of 6,7,8,9-tetrahydro-5H-5-hydroxy phenyl thiazolo (2,3-b) quinazolin-3(2H)-one with appropriate hydrazine hydrate and ketones/aldehydes in the presence of anhydrous sodium acetate and glacial acetic acid as presented in Scheme 1. Their antinociceptive activity were evaluated by tailflick technique, anti-inflammatory was evaluated by carrageenan-induced paw edema test and their ulcerogenicity index determined by reported protocol. The compounds exhibited the lowest ulcer index ($0.51{\pm}1.63$, $0.48{\pm}1.28$ and $0.50{\pm}1.53$, respectively. The 6,7,8,9-tetrahydro-5H-5-hydroxy phenylhydroxy-2-benzylidine-3-(N'-3-pentylidenehydrazino) thiazolo (2,3-b) quinazoline and 6,7,8,9-tetrahydro-5H-5-hydroxy phenyl-2-benzylidine-3-(N'-2-pentylidene-hydrazino) thiazolo (2,3-b) quinazoline exhibited the most potent antinociceptive and anti-inflammatory activities.

Reactions of Pyrimidinonethione Derivatives;Synthesis of 2-Hydrazinopyrimidin-4-one, Pyrimido[1,2-a]-1,2,4-triazine, Triazolo-[1,2-a]pyrimidine, 2-(1-pyrazolo)Pyrimidine and 2-Arylhydrazonopyrimidine Derivatives

  • Attaby, Fawzy-A.;Eldin, Sanaa-M.;Hanafi, Eman-A.Z.
    • Archives of Pharmacal Research
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    • v.20 no.6
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    • pp.620-628
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    • 1997
  • 6-Aryl-5-cyano-4-pyrimidinon-2-thione derivatives 1a-c reacted with ethyl iodide to give the corresponded 2-S-ethylpyrimidin-4-one-derivatives 2a-c. Compounds 2a-c was, in turn, reacted with hydrazine hydrate to give the sulfur free reaction products, 3a-c. These reaction products were taken as the starting materials for the synthesis of several newly synthesized heterocyclic derivatives. Reactions with several halogenated ketones, esters, chloroacetic acid and chloroacetamide give pyrimidotriazines 8,12 and 15 while their reactions with formic acid, acetic acid and carbon disulfide gave the corresponded triazolopyrimidines 17 and 21. The reaction with both acetyl acetone and ethylacetoacetate gave the corresponded 2-$(3^{I},5^{I}-dimethyl-1^{I}-pyrazoly$pyrimidine derivatives 20a-c and 24a-c respectively while the reaction with cinnamonitriles 25a-h afforded the corresponded aryl hydrazopyrimidines 27a-f. The structure of these reaction products were eatablished based on both elemental anlayses and spectral data studies.

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