• 제목/요약/키워드: Cyclisation

검색결과 8건 처리시간 0.022초

Synthesis of Novel Series of Various Substituted1-(5-(2-p-tolyloxyquinolin-3-yl)-2-(pyridin-4-yl)-1,3,4-oxadiazol-3(2H)-yl)ethanone and its Antibacterial Activity

  • Joshi, Ratnadeep S.;Mandhane, Priyanka G.;Chate, Asha V.;Gill, Charansingh H.
    • 대한화학회지
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    • 제55권5호
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    • pp.760-764
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    • 2011
  • A new series of 1-(5-(2-tolyloxyquinoline-3-yl)-2-(pyridine-4-yl)-1,3,4-oxidiazol-3(2H)-yl)ethanones were synthesized from cyclisation of N'-((2-(p-tolyloxy)quinoline-3-yl)methylene) isonitonohydrazide in acetic unhydride at reflux condition for 3-4 hr. The structures of the new compounds were confirmed by elemental analyses as well as IR, 1H NMR and mass spectral data. All the synthesized compounds were screened for their antibacterial activities against various bacterial strains. Several of these compounds showed potential antibacterial activity.

Peracetylated N-Lactosyl-1,2,4-Thiadiazolidin-3-one Hydrochlorides: 합성과 항균 연구 (Novel Peracetylated N-Lactosyl-1,2,4-Thiadiazolidin-3-one Hydrochlorides: Synthesis and Antimicrobial Studies)

  • Dandale, Anvita S.;Mangte, Dattatraya V.;Deshmukh, Shirish P.
    • 대한화학회지
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    • 제54권3호
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    • pp.287-290
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    • 2010
  • Peracetylated lactosyl carbamides와 N-phenyl-S-chloro isothiocarbamoyl chloride를 고리화 반응을 시켜서 peracetylated N-Lactosyl-1,2,4-thiadiazolidin-3-one hydrochlorides를 합성하였으며, 얻어진 화합물을 이용하여 bacteria S. aureus, E. coli, P. Vulgaris, P. Aeruginosa and fungi A. Niger, Penicillium 항균 활성을 연구하였다.

Studies on Synthesis and Heterocyclisation Reactions of Michael Products and Formation of New 1, 4-Thiazine Quinoxaline Derivatives

  • Mahgoub, S.A.
    • Archives of Pharmacal Research
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    • 제13권4호
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    • pp.319-324
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    • 1990
  • Synthesis of $\alpha$-piperidino and $\alpha$-morphelino styryl quinoxalinone 2f, 2g respectively by facile one step method is reported. The Michael adducts (3a-d) obtained by the interaction of 2-styryl-2 (1H) quinoxalinone (2) and ethylacetoacetate have been treated with resorcino and hydroxylamine separately. With resorcinol the chromones (4) are obtained whereas with ydroxylamine isoxazoles (6) are the products. Michael addition of acetylacetone to 2 leads to 3-[1'-aryl-2'-(2'-hydroxy-3'-quinoxalinyl)ethyl]-2, 4-pentanediones (5) which undergo cyclisation with hydroxylamine to give isoxazoles (7). Addition of thiopenol and thioglycolic acid to 2 gives 3-$\alpha$[$\beta$-(phenyl)-$\beta$-(plenylthio)]ethyl-2(1H)-quinoxalinone (8) and 3-$\alpha$-[$\beta$-phenyl)-$\beta$-(hydroxycarbonylmethylithio)]-ethyl-2(1H)-qui noxalinone (9) respectively. 2-Bromomethyl-2(1H)-quinoxalinone (1b) reacts with thioglycolic acid to gives S-[2 (1H)-oxoquionoxaline-3-yl-methyl] mercaptoacetic acid (10) which on cyclisation with acetic anhydride/pyridine affords 1, 2, 5, 6-tetrahydro [1, 4]thiazino[4, 3-a] quinoxaline-1, 6-dione (11).

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Reactions with Acetoacetanilide : Synthesis and antibacterial activity of some new pyran, pyrano [2, 3-clpyrazole and pyrano [2, 3,-c]-pyridine deerivatives

  • Y, Riad-Bahia;O, Abdelhamid-Abdou;Khalifa, Fathy-A;E, Saleh-Youssry
    • Archives of Pharmacal Research
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    • 제12권3호
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    • pp.201-206
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    • 1989
  • The reaction of acetoacetanilide (1) with the $\alpha$-cyanocinnamonitrile derivatives 2 yielded the Michael adducts 4 which could be converted into the pyrano [2, 3, -c] pyrazole derivatives 5 via their reaction with hydrazine hydrate. Cyclisation of 4 afforded the derivatives 10. The pyranopyrazoles 9 reacted with different activated nitrile derivatives (3a-c) to give the pyrano [2, 3-c] pyridine derivatives 13. 16 and 19 respectively. The biological activity of the synthesised heterocyclic derivatives was investigated and discussed.

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Design, Synthesis, Fluorescence Properties and Antibacterial Activities of New 8-Chloro-3-Alkyl-3H-Pyrazolo[4,3-a]acridine-11-Carbonitriles

  • Rahmani, Zeynab;Pordel, Mehdi;Davoodnia, Abolghasem
    • Bulletin of the Korean Chemical Society
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    • 제35권2호
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    • pp.551-556
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    • 2014
  • The treatment of alkylated nitro derivatives of indazole with 2-(4-chlorophenyl)acetonitrile under basic conditions gave the new 8-chloro-3-alkyl-3H-pyrazolo[4,3-a]acridine-11-carbonitriles via the nucleophilic substitution of hydrogen which proceeds at room temperature with concomitant cyclisation in fairly good yields. The structures of all newly synthesized compounds were confirmed by IR, $^1H$ NMR, $^{13}C$ NMR and mass spectral data. Fluorescence experimental results of all newly synthesized compounds revealed remarkable photoluminescence properties and strong green fluorescence properties. Also, the new compounds exhibited potent antibacterial activity and their antibacterial activity (MIC) against Gram positive (Staphylococcuse aureus methicillin resistant S. aureus and Bacillus subtilis) and negative bacterial (Pseudomonas aeruginosa and Escherichia coli) species were determined.

Oxidative Cyclisation Based One-Pot Synthesis of 3-Substituted[1,2,4]triazolo[4,3-b]pyridazines Using Me4NBr/Oxone

  • Ruso, Jayaraman Sembian;Nagappan, Rajendiran;Kumaran, Rajendran Senthil
    • 대한화학회지
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    • 제57권5호
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    • pp.606-611
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    • 2013
  • A facile one-pot syhthesis of 3-substituted triazolopyridazine and thieno-triazolopyridazine derivatives is described. This protocol involves the preparation of heteroaryl hydrazone from the aldehyde and pyridazinohydrazine derivative followed by subjecting the intermediate directly to oxidative cyclization to assemble the desired 1,2,4-triazloe moiety by employing the mixture of Me4NBr and oxone. This condition is efficient and is able to tolerate wide range of functional groups.

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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    • 제13권3호
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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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Pyrazole과 Pyrazolotriazole 유도체의 합성 및 특성 연구 (Synthesis, Fastness and Spectral Properties of Some New Azo Pyrazole and Pyrazolotriazole Derivatives)

  • Rizk, Hala F.;El-Badawi, Mahmoud A.;Ibrahim, Seham A.;El-Borai, Mohamed A.
    • 대한화학회지
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    • 제54권6호
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    • pp.737-743
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    • 2010
  • 5-Amino-1,3-diaryl-pyrazoles 1a-c 와 다양한 aryl amine의diazonium salts를 반응시켜서 1,3-diaryl-5-amino-4-arylazopyrazoles 3a-l을 합성하였으며, 몇 가지 화합물은 5-amino-1,3-diaryl-4-nitroso-1H-pyrazoles 2a-c와 aryl amine의 diazonium salts를 반응시켜서 얻었다. 합성한 azo 유도체 화합물 3a-l을 DMF 용매 속에서 cupric acetate와 산화반응시켜서 2,4,6-triaryl-2,4-dihydropyrazolo [4,3-d]-1,2,3-triazoles 4a-l을 합성하였으며, 합성한 cyclic triazoles에 대한 형광 특성을 측정하였다. 한편, Diazotization of sodium nitrite/ortho-phosphoric acid 조건에서 5-amino-1,3-diaryl-1H-pyrazoles 1a-c를 diazotization화 반응시킨 다음에, aryl amines과 반응시켜서 o-aminoazo compounds 5a-f를 합성하였다. 합성한 화합물 5a-f를 pyridine/cupric acetate 반응 조건에서 반응시켜서 triazole 6a-f들을 합성하였으며, 얻어진 화합물 6a-f을 aryl diazonium salts과 반응시켜서 화합물 7a-j을 합성하였다. 합성한 염료 화합물을 polyesters에 분산염료와 정착성을 측정하였다.