• Title/Summary/Keyword: 1,3-dicyclohexylcarbodiimide

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Cyclocondensation of 2-Substituted-4-hydroxy-2H-1, 2-benzothiazine-3-carboxylic acid 1, 1-dioxides with Dicyclohexylcarbodiimide (2-치환 4-Hydroxy-2H-1, 2-benzothiazine-3-carboxylic acid 1, 1-dioxidies와 Dicyclohexylcarbodiimide의 축합환화 반응)

  • 서정진;홍유화
    • YAKHAK HOEJI
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    • v.31 no.1
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    • pp.40-41
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    • 1987
  • 4-Hydroxy-2H-1, 2-benzothiazine-3-carboxylic acid 1a was reacted with 2 equivalents of dicyclohexylcarbodiimide (DCC) to give 2-cyclohexyl-3-cyclohexylimino-4,5-dihydro-1H-imidazo [1,5-b][1,2] benzothiazine-10, 10a-dyhydro-1,10-dione 5,5-dioxide 2a and dicyclohexylurea (DCU). On the other hand 2-substituted-4-hydroxy-2H-1, 2-benzothiazine-3-carboxylic acid 1,1-dioxide 1b or c was reacted with DCC to give 2-cyclohexylimino-3-cyclohexyl-5-alkyl-4-oxo-2,5H-1,3-oxazino [5,6-c]-1,2-benzothiazine 6,6-dioxide 2b or c and DCU.

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Synthesis of New Benzimidazo [2,1-b][1,3,5]benzothiadiazepine Derivatives (새로운 Benzimidazo[2,1-b][1,3,5]benzothiadiazepine 유도체들의 합성)

  • Jin, Byeong U;Jo, Seong Hui
    • Journal of the Korean Chemical Society
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    • v.38 no.5
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    • pp.382-390
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    • 1994
  • New 6-imino-5H-benzimidazo[2,1-b][1,3,5]benzothiadiazepine derivatives (8) were successfully synthesized in good yields from the N-[2-(benzimidazol-2-yl thio)phenyl]thiourea derivatives (6) in the presence of dicyclohexylcarbodiimide(DCC) and from N-[2-(benzimidazol-2-yl thio)phenyl]-S-methylisothiourea derivatives (7) with potassium carbonate.

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Study on the Synthesis of N,N'-Dicyclohexylcarbodiimide from N,N'-Dicyclohexylurea (디사이클로헥실우레아로부터 디사이클로헥실카르보디이미드의 합성에 관한 연구)

  • Kim, Jae Young;Chung, Dae-Won
    • Applied Chemistry for Engineering
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    • v.22 no.3
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    • pp.319-322
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    • 2011
  • N,N'-Dicyclohexylcarbodiimide (DCC) known as powerful dehydrating reagent in amide or ester synthesis is converted into N,N'-dicyclohexylurea (DCU) during the reaction. In the paper, DCU was recovered from the reaction for the synthesis of the hydrophilic derivative of ${\beta}$-sitosterol, and the purification of the recovered DCU and the dehydration of DCU into DCC were investigated. In the presence of tosyl chloride, (TsCl) and triethylamine (TEA), DCU was converted into DCC, and the optimum molar ratio of [DCU] : [TsCl] : [TEA] was found to be 1.0 : 1.5 : 3.0. Pure DCC was obtained with a 46% yield by the sublimation after the purification process, and characterized by GC/MS, FT-IR and $^{13}C-NMR$.

Synthesis of Potential Antiinfammatory Benzisothiazoline Derivatives (잠재성 항염효과가 있는 벤즈이소티아졸린 유도체의 합성)

  • 박명숙;윤명선;김미경;권순경
    • YAKHAK HOEJI
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    • v.45 no.6
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    • pp.570-574
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    • 2001
  • In order to discover new useful NSAIDs, novel N-substituted 1,2-benzisothiazoline-3-one 1,1- dioxide derivatives, which can exhibit potentially antiinflammatory activity were synthesized. 1,2-Benz-isothiazoline-3-one-N-acetic acids 6a, b were obtained from monochloroacetic acid and sodium 1,2-benz-isothiazoline-3-ones in DMF by N-alkylation reaction. N-Substituted 1,2-benzisothiazoline-3-one 1,1-dioxide derivatives 7a-e were synthesized through the coupling of compound 6a, b and several amines (aniline, 2- aminopyridine , 2-aminothiazole, 2-aminotetrazole) with dicyclohexylcarbodiimide in methyl e no chloride.

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Preparation and Characteristics of Surface-Modified Albumin Microspheres with Methotrexate (메토트렉세이트가 표면수식된 알부민 미립구의 제조 및 특성)

  • Hwang, Sung-Joo;Jo, Hang-Bum;Rhee, Gye-Ju;Kim, Chong-Kook
    • Journal of Pharmaceutical Investigation
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    • v.25 no.2
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    • pp.101-108
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    • 1995
  • The surface of albumin microspheres could be modified with methotrexate (MTX) by using 1,3-dicyclohexylcarbodiimide (DCC). Surface-modified albumin microspheres entrapping no MTX (SAMS), free MTX (SAMSF) and MTX-bovine serum albumin (BSA) conjugates (SAMSC) were prepared. respectively, and their release characteristics were investigated in the presence of trypsin using a dissolution tester. The mean diameters of all the microspheres were $5{\sim}8\;{\mu}m$, and their shapes was small and uniform. MTX bound tn their surfaces was released slower than the entrapped free MTX, and laster than the entrapped MTX-BSA conjugates. Also, surface-modified MTX was scarcely released in the absence of a proteolytic enzyme. Therefore, the surface-modified MTX may be released rapidly from SAMSC at the target site, and thereafter MTX may be released slowly from the encapsulated MTX-BSA conjugates in SAMSC for a long period.

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A facile synthesis of (E)-2-hexenyl (E)-2-hexenoate and (E)-2-hexenyl (Z)-3-hexenoate, pheromone components of Riptortus pedestris (톱다리개미허리노린재 페로몬, (E)-2-hexenyl (E)-2-hexenoate과 (E)-2-hexenyl (Z)-3-hexenoate의 합성)

  • Kim, Junheon;Park, Chung Gyoo
    • The Korean Journal of Pesticide Science
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    • v.17 no.2
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    • pp.140-143
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    • 2013
  • We investigated optimal condition for synthesis of (E)-2-hexenyl (E)-2-hexenoate (1) and (E)-2-hexenyl (Z)-3-hexenoate (2), the pheromone components of Riptortus pedestris, by Steglich esterification. The reaction with 1.1-1.5 equivalent of dicyclohexylcarbodiimide (DCC), 1.5-2.0 equivalent of (E)-2-hexenol, and 0.1 equivalent 4-dimethylaminopyrinde (DMAP) to (E)-2-hexenoic acid in toluene or (Z)-3-hexenoic acid in dichloromethane led 1 and 2 in 76-78% and 87-91% yield, respectively.

Properties and Hair-growth Effect of Chrysin 7-O-crotonate (크라이신 7-O-크로토네이트의 물성 및 육모효과)

  • 신준수;김연희;정재훈;김양배;김박광
    • YAKHAK HOEJI
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    • v.43 no.3
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    • pp.316-319
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    • 1999
  • Chrysin 7-Ο-crotonate was synthesized by condensing crotonic acid with chrysin in organic solvent, tetrahydrofuran (THF) using dicyclohexylcarbodiimide (DCC) and 4-dimethylaminopyridine (DMAP). Its structure was indentified by NMR, MS, UV, IR etc. We also investigated the physico-chemical properties and set up the quantitative anytical method of this compound. The correlation coefficient of calibration curve measured at the isobestic point (340 nm) on this compound was approximately 0.9994 by absorption spetrophtometry. Detection limit was 1.6ng at S/N=3 by using a RP column by HPLC. The hair growth effect fo chrysin 7-Ο-crotonate on the hair of black mouse (C57BL/6), was carried out using paste method. When its ethanol solution was administered to this black mouse by route of skin, this compound promoted the growth of hair.

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Characterization of the Membrane Potential Relevant to Permeability Changes in the Plasmalemma of Lemna gibba G3 (좀개구리밥 (Lenma gibba G3)의 원형질막의 투과성 변화와 관련된 막전위의 특성)

  • 윤병길
    • Journal of Plant Biology
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    • v.33 no.2
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    • pp.135-140
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    • 1990
  • The membrane potential in the subepidermal cells of Lemna gibba G3 fronds was measured in the dark with glass capillary microelectrodes. At pH 7, the membrane potential, approximately-215 mV, could be depolarized to -82∼-88 mV by 0.1 mM dicyclohexylcarbodiimide (DCCD) or by KCN at 0.3 mM or higher concentrations. When the pH of the medium was altered the potential showed reversible changes, while it revealed no response to the external pH changes when energy transduction across the membrane was being blocked by 0.1 mM DCCD. The results support an assumption that the active component of the membrane potential of Lemna subepidermal cells is generated by electrogenic H+ -pump. By the addition of 0.10∼5.00 mM salicylic acid(SA) to the bathing medium the membrane potential was depolarized to a great extent, and the removal of SA from the medium repolarized the potential showing almost complete recovery, 92.3∼97.6% to the initial levels. Although the potential was greatly depolarized by 5.0% or higher concentrations of dimethylsulfoxide (DMSO), the recovery rate by DMSO removal was decreased as the pretreatment concentration had increased. Twenty percent DMSO pretreatment limited the recovery at only 47.1%. The presence of SA in the bathing medium could reversibly increase the permeability of the plasmalemma. DMSO at its concentration of 5.0% or higher increased the permeability of the membrane by irrevesibly impairing the membrane component involved in the membrane permeability.

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Characteristics of ATPases Present in Everted Membrane Vesicles of Helicobacter pylori

  • Yun, Soon-Kyu;Hwang, Se-Young
    • Journal of Microbiology and Biotechnology
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    • v.7 no.3
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    • pp.167-173
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    • 1997
  • Everted membrane vesicles of Helicobacter pylori were prepared and the membrane-resided ATPases were characterized. For comparison, Escherichia coli membrane ATPases and hog gastric mucosal H,K-ATPase were employed. ATPase assay revealed that the composite enzyme pool was relatively low in specific activities, below 1/10 times than that found in E. coli. According to their inhibitory specificities, most of the ATPase pool appeared to belong to the P-type ATPase, sensitive to vanadate but not to azide. The enzyme pool was extraordinarily resistant against treatment by N,N'-dicyclohexylcarbodiimide (DCCD). Certain monovalent cations, e.g., $K^+$ or $NH_4^{+}$ stimulated the whole enzyme pool only in the presence of $Mg^{2+}$. On the contrary, $Ni^{2+}$ and $Zn^{2+}$ increased enzyme activity rather effectively without the aid of $Mg^{2+}$. Under a defined condition employed, H. pylori cells could retain the membrane ATPase pool to the extent of $17{\%}$ at pH 3.2. Moreover, its activity was most stable in acidic conditions (pH 5.4-6.4). However, cytoplasmic or peripheral ATPase pools were hardly detected under acidity (below pH 4.6).

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