• 제목/요약/키워드: intermediate compound

검색결과 133건 처리시간 0.026초

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

  • 한영택
    • 약학회지
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    • 제59권2호
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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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    • 제31권7호
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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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    • 제19권2호
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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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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) (Growth and Physiological Responses of Shade Intolerant and Intermediate Tree Seedlings to Enhanced UV-B Radiation)

  • 김종진;홍성각
    • 한국산림과학회지
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    • 제88권4호
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    • pp.469-476
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    • 1999
  • 본 연구는 증가되는 UV-B 환경에 대한 양수(陽樹)와 중성수(中性樹)의 생장 및 생리적 반응을 탐구하고자 자작나무(Betula platyphylla var. japonica Hara)와 물푸레나무(Fraxinus rhynchophylla Hance)의 유묘(幼苗)를 대상으로 14주 동안 3 수준의 UV-B(ambient UV-$B_{BE}$, ambient+3.2, +$5.2\;KJ\;m^{-2}s^{-1}$) lamp가 설치된 야외포장에서 실시되었다. 자작나무와 물푸레나무 유묘의 수고생장(樹高生長), 근원경생장(根元徑生長), 엽면적(葉面積) 및 건물생산(乾物生産)은 UV-B 증가에 의하여 감소되었다. UV-B 증가에 의해 물푸레나무 유묘 잎의 기공저항(氣孔低抗)은 커졌으며, 엽록소(葉綠素), carotenoid 함량의 감소는 자작나무에서 보다 물푸레나무에서 더 뚜렷하였다. UV-B 흡수물질(吸收物質)의 현저한 증가는 나타나지 않았지만 자작나무에 비해 물푸레나무의 경우 다소 증가하는 경향이었다. 이러한 결과들은 UV-B 증가 환경에 대한 공시 두 수종의 생리적(生理的), 생화학적(生化學的) 반응이 다르다는 것을 의미한다.

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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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    • 제8권1호
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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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    • 제6권2호
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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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Ti-51.5at.%Ni 형상기억합금 단결정의 소성변형 거동 (Plastic Deformation Behavior of Ti-51.5at.%Ni Shape Memory Alloy Single Crystals)

  • 전중환
    • 열처리공학회지
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    • 제15권1호
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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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    • 한국신재생에너지학회 2009년도 춘계학술대회 논문집
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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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    • 제28권11호
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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.

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

  • 권민정;최윤호;송상환;박혜연;구현주;박광식
    • Environmental Analysis Health and Toxicology
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    • 제16권4호
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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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