• Title/Summary/Keyword: intermediate compound

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Concise Synthesis of Flurbiprofen via Palladium-Catalyzed Cross-Coupling Reactions (팔라듐 촉매하 결합반응을 이용한 플루비프로펜의 간결한 합성)

  • Han, Young Taek
    • YAKHAK HOEJI
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    • v.59 no.2
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    • pp.66-69
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    • 2015
  • A concise synthesis of flurbiprofen, a member of the non-steroidal anti-inflammatory 2-arylpropionic acids, has been accomplished. The key feature of this synthesis involves successive palladium-catalyzed cross coupling reactions. In particular, a 2-arylacylate intermediate, which easily converted to the key 2-arylpropionic acid scaffold, was afforded by a versatile palladium-catalyzed cross coupling reaction between diazopropanate and bisphenylboronic acid. This synthetic procedure would facilitate synthesis of the flurbiprofen and anti-inflammatory 2-arylpropionic acid derivatives.

New Phenylaminopyrimidine (PAP) Anticancer Lead Compound with High Efficacy: Design, Synthesis, and in vitro Screening

  • El-Deeb, Ibrahim Mustafa;Han, Dong-Keun;Kim, In-Tae;Lee, So-Ha
    • Bulletin of the Korean Chemical Society
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    • v.31 no.7
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    • pp.1848-1858
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    • 2010
  • Phenylaminopyrimidines represent a large group of new selective anticancer agents, the majority of which exert their action through the inhibition of specific kinases. In this study, a new series of N-substituted-2-aminopyrimidines has been designed and synthesized. A selected group of the synthesized derivatives was screened at a single dose concentration of 10 ${\mu}M$ over a panel of 60 cancer cell-lines. Compound 12e has showed great inhibitory and strong lethal effect over almost all of the 60 cell-lines and accordingly was further tested in a 5-dose testing mode to determine its $IC_{50}$ values, where it showed great efficacies with intermediate potencies over the tested cell-lines. The compound was also tested over a panel of 52 kinases to explore its kinase inhibitory profile, and was found to be a selective but moderate inhibitor over FLT3 kinase.

Effects of newly synthesized benzimidazole derivatives on gastric H^+/K^+$ ATPase

  • Cheon, Hyae-Gyeong;Yum, Eul-Kgun;Kim, Sung-Soo
    • Archives of Pharmacal Research
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    • v.19 no.2
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    • pp.126-131
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    • 1996
  • The effects of various synthetic benzimidazole derivatives on gastric H^+/K^+$ATPase activity in vitro were examined. The results showed that the effects of substituents on the benzimidazole ring were not significant. However, replacement of sulfoxide connecting two ring systems to sulfide resulted in a completely inactive compound in vitro, suggesting the essential role of sulfoxide group in the inhibition. In addition, compounds with 5 or 6-membered oxacyclic substituents attached to the pyridine ring displayed the most effective inhibitory activity. Among these derivatives, AU-47 was the most potent, and detailed mechanistic studies with the compound were carried out. AU-47 inhibited gastricH^+/K^+$ATPase in a concentration and time dependent manner with 50% inhibition at $6\muM$. The presence of sulfhydryl reducing agents or substrate analogue protected H^+/K^+$ATPase from the inactivation. The inhibition by AU-47 was potentiated by acid pretreatment of the compound, suggesting the structural conversion of AU-47 into a more active intermediate which was favored in acidic condition. Consistent with in vitro results, AU-47 inhibited in vivo gastric acid secretion. The results suggest that AU47 is a relevant candidate for the development of new antiulcer agent.

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Growth and Physiological Responses of Shade Intolerant and Intermediate Tree Seedlings to Enhanced UV-B Radiation (자외선(紫外線)-B 증가조사(增加照射)에 대한 양수(陽樹)와 중성수(中性樹) 유묘(幼苗)의 생장(生長)과 생리적(生理的) 반응(反應)에 관한 연구(硏究))

  • Kim, Jong Jin;Hong, Sung Gak
    • Journal of Korean Society of Forest Science
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    • v.88 no.4
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    • pp.469-476
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    • 1999
  • This study was carried out to investigate the growth and physiological response of shade intolerant and intermediate tree seedlings to enhanced UV-$B_{BE}$(biologically effective UV-B) radiation. The seedlings of Betula platyphylla var. japonica Hara(shade intolerant species) and Fraxinus rhynchophylla Hance(shade intermediate species) were treated with one of the three levels of UV-$B_{BE}$ dosages - ambient UV-$B_{BE}$, ambient+3.2, and ambient+$5.2\;KJ\;m^{-2}day^{-1}$) for 14 weeks in the field condition. Height and root collar diameter growth, leaf area, and biomass production of the seedlings of two species were reduced by enhanced UV-B radiation. Leaf stomatal resistance to water vapor of the F. rhynchophylla seedling was increased by the UV-B increment. The reductions in total chlorophyll and carotenoid were more apparent in the F. rhynchophylla than B. platyphylla seedling. There was no statistically significant changes in the concentration of UV-B absorbing compound($A_{300}$) in the leaves of the two species among the UV-B treatment. However the $A_{300}$ tented to be increased in F. rhynchophylla by enhanced UV-B radiation. These results indicate that the growth and the physiological and biochemical responses between B. platyphylla and F. rhynchophylla were different to enhanced UV-B environment.

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Recent developments and challenges in welding of magnesium to titanium alloys

  • Auwal, S.T.;Ramesh, S.;Tan, Caiwang;Zhang, Zequn;Zhao, Xiaoye;Manladan, S.M.
    • Advances in materials Research
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    • v.8 no.1
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    • pp.47-73
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    • 2019
  • Joining of Mg/Ti hybrid structures by welding for automotive and aerospace applications has attracted great attention in recent years due mainly to its potential benefit of energy saving and emission reduction. However, joining them has been hampered with many difficulties due to their physical and metallurgical incompatibilities. Different joining processes have been employed to join Mg/Ti, and in most cases in order to get a metallurgical bonding between them was the use of an intermediate element at the interface or mutual diffusion of alloying elements from the base materials. The formation of a reaction product (in the form of solid solution or intermetallic compound) along the interface between the Mg and Ti is responsible for formation of a metallurgical bond. However, the interfacial bonding achieved and the joints performance depend significantly on the newly formed reaction product(s). Thus, a thorough understanding of the interaction between the selected intermediate elements with the base metals along with the influence of the associated welding parameters are essential. This review is timely as it presents on the current paradigm and progress in welding and joining of Mg/Ti alloys. The factors governing the welding of several important techniques are deliberated along with their joining mechanisms. Some opportunities to improve the welding of Mg/Ti for different welding techniques are also identified.

Effect of the Supplement of Metabolites on Cell Growth and Poly-$\beta$-hydroxybutyrate Biosynthesis of Alcaligenes latus

  • Lee, Yong Hyun;Tae Woo Kim;Jin Seo Park;Tae Lin Huh
    • Journal of Microbiology and Biotechnology
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    • v.6 no.2
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    • pp.120-127
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    • 1996
  • The characteristics of cell growth and poly-$\beta$-hydroxybutyrate biosynthesis of Alcaligenes latus ATCC 29713 were investigated. The PHB accumulation pattern of A. latus followed a growth-associated type where the cell growth and PHB accumulation were carried out simultaneously. Various intermediate compounds such as metabolites involved in the TCA cycle, amino acids, and saturated and unsaturated fatty acids were added to examine their effect on cell growth and PHB accumulation. Citrate, tyrosine, and palmitic acid showed the most significant increase both on cell growth and PHB accumulation. Maximum PHB concentrations were noticeably increased about 1.4 to 1.6 times higher than that of control, corresponding to 5.54, 6.45, and 6.45 g/l for citrate, tyrosine, and palmitic acid, respectively. The stimulatory effects of the supplemented metabolites were analyzed in terms of the increment of enzyme activities related to sugar catabolism and PHB biosynthesis.

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Plastic Deformation Behavior of Ti-51.5at.%Ni Shape Memory Alloy Single Crystals (Ti-51.5at.%Ni 형상기억합금 단결정의 소성변형 거동)

  • Jun, Joong-Hwan;Sehitoglu, Huseyin
    • Journal of the Korean Society for Heat Treatment
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    • v.15 no.1
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    • pp.9-15
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    • 2002
  • Deformation behavior of nickel-rich Ti-51.5at.%Ni single crystals was investigated over a wide range of temperatures(77 to 440K) and strain levels(up to 9%) in compression. These alloys combined superior strength with wide range of pseudoelasticity temperature interval(~200K). The slip deformation in [001] orientation did not occur due to the prevailing slip system, and consequently, exhibited pseudoelastic deformation at temperatures ranging from 77 to 283K and 273 to 440K for the solutionized and over-aged cases, respectively. The critical transformation stress levels were in the range of 800 to 1800MPa for the solutionized case, and 200 to 1000MPa for the over-aged case depending on the temperature and specimen orientation. These stress levels are considerably higher compared to these class of alloys having lower Ni contents. The maximum transformation strains, measured from incremental straining experiments in compression, were lower compared to the phenomenological theory with Type II twinning. A compound twinning model depending on the successive austenite(B2) to intermediate phase(R) to martensite(B19') transformation predicts lower transformation strains compared to the Type II twinning case.

Synthesis of $Cu_2ZnSnSe_4$ compound by solid state reaction using elemental powders

  • Wibowo, Rachmat Adhi;Alfaruqi, Muhammad H.;Jung, Woon-Hwa;Kim, Kyoo-Ho
    • 한국신재생에너지학회:학술대회논문집
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    • 2009.06a
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    • pp.134-137
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    • 2009
  • Commercially available elemental powders of Cu, Zn, Sn and Se were employed for crystallizing a stannite-type $Cu_2ZnSnSe_4$ compound by means of solid state reaction. $Cu_2ZnSnSe_4$ reaction chemistry was also modeled based on differential-thermal analysis and X-ray powder diffraction results. It was observed that Se tends to react preferably with Cu to form CuSe and $CuSe_2$ phases at low reaction temperature. The formation of $Cu_5Zn_8$ intermetallic phase was found to be the intermediate reaction path for the binary ZnSe formation. A solid state reaction at $320^{\circ}C$ reacted elemental powderst obinary selenides of CuSe, ZnSe and SnSe completely. The crystallization of $Cu_2ZnSnSe_4$ was was detected to begin at $300^{\circ}C$ and its weight fraction increased with an increase of reaction temperature, which most probably formed from the reaction between $Cu_2SnSe_3$ and ZnSe.

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Synthesis of New 2-Thiouracil-5-Sulphonamide Derivatives with Antibacterial and Antifungal Activity

  • Fathalla O. A.;Awad S. M.;Mohamed M. S.
    • Archives of Pharmacal Research
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    • v.28 no.11
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    • pp.1205-1212
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    • 2005
  • 2-Thiouracil-5-sulphonic acid N-(4-acetylphenyl) Amide (1) was reacted with a series of aromatic aldehydes giving chalcones 2 (Claisen-Schemidt reaction), some of these chalcones were reacted with urea and thiourea giving pyrimidine-2-one and pyrimidine-2 thione derivatives respectively of the type 3a,b and 4a,b. In addition many chalcones were reacted with hydroxylamine hydrochloride giving isoxazoline derivatives 5a,b. They could also reacted with phenylhydrazine to give pyrazoline derivatives 5a,b, chalcones also were reacted withethylcyano acetate and/or malononitryl in pyridine giving pyran derivatives 7a,c and 8a,c. In another pathway chalcones were epoxidised by $H_{2}O_{2}$ giving epoxides 9a,c which in turn were reacted with phenylhydrazine giving 4-hydroxypyrazoline derivatives 10a,c. In another reaction chalcones were reacted with ethylcyanoacetate in presence of amm.acetate giving pyridone derivatives 11a,d which could be prepared also in exellent yield from compound 1 by its reaction with certain aromatic aldehydes and ethylcyanoacetate in presence of ammonium acetate. Finally, compound 1 was reacted with semicarbazide giving semicarbazone intermediate 12 which in turn was reacted with thionyl chloride giving thiadiazole derivative 13. The biological effects of some of the new synthesized compounds were also investigated.

Estimated Bioaccumulation properties of Acetanilide using BCFWIN (BCF WIN을 이용한 Acetanilide의 생물농축특성 평가)

  • Kwon, Min-Jeong;Choi, Yoon-Ho;Song, Sang-Hwan;Park, Hye-Youn;Koo, Hyun-Ju;Park, Kwang-Sik
    • Environmental Analysis Health and Toxicology
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    • v.16 no.4
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    • pp.223-226
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    • 2001
  • Acetanilide is a High Production Volume Chemical, which is produced about 2,300 tons/year in Korea as of 1998 survey. Most is used as an intermediate for synthesis of pharmaceuticals and dyes. The chemical is one of seven chemicals, which are under the frame of OECD SIDS program sponsored by National Institute of Environmental Research of Korea. Regarding the information on the environmental fate. bioconcentration is one of important factor to estimate the environmental tranfer. However, measurement of bioconcentration needs high expense and time. For this reason, OECD recommends to use BCFWIN model to estimate bioconcentration of organic chemicals, BCFWIN estimates the bioconcentration factor (BCF) of an organic compound using the log octanol-water partition coefficient (Kow) of the compound. Structures are entered into BCFWIN through SMITES (Simplified Molecular Input Line Entry System) notations. The BCFWIN method classifies a compound as either ionic or non-ionic. ionic compounds include carboxylic acids, sulfonic acids and salts of sulfonic acids, and charged nitrogen compounds (nitrogen with a + 5 valence such as quaternary ammonium compounds). All other compounds are classified as non-ionic. In this study, bioaccumulation of acetanilide was estimated using BCFWIN model based on SMIIES notation, chemical name data and partition coefficient as one of environmental fate/distribution of the chemical elements.

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