• Title/Summary/Keyword: 7-epoxide

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Synthesis of 10-Oxo-$\beta$-rhodomycinone Derivatives

  • Rho, Young S.;Kim, Sun Y.;조인호;강흠수;유동진;정채준
    • Bulletin of the Korean Chemical Society
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    • v.19 no.10
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    • pp.1059-1063
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    • 1998
  • Regiospecific total syntheses of (±)-11-deoxy-4-methoxy-10-oxo-βrhodomycinone (21a) and (±)-11-deoxy-1-methoxy-10-oxo-β-rbodomycinone (21b) are described. 2-(2-Bromoethyl)-1,3-dioxane (6) was transformed to naphthalenone 12, which was condensed with (phenylsulfonyl)-isobenzofuranone 13 to afford 7,8-dihydro-9-ethyl-6-hydroxy-4-methoxynaphthacen-5,12-dione (15). Epoxide 16 prepared from olefinic compound 15, reacted with HF/Pyr (7:3) to give 17. Dihydroxylation of 17 with t-BuOK/P(OMe)3/O2, selective cis-diol protection of mixed compounds 18 with phenylboronic acid in toluene, separation of cis-boronate 19 and trans-diol 20 by column chromatography on silica gel, and cleavage of the boronate group of 19 with 2-methylpentane-2,4-diol in acetic acid completed the construction of 21.

Studies on the Residues of Chlorinated Organic Insecticides - I. Heptachlor Residues in or on Commercial Vegetables - (유기염소계(有機鹽素系) 살충제(殺蟲劑)의 잔류분(殘留分)에 관(關)한 연구(硏究) - 1. 시판채소중(市販菜蔬中) Heptachlor 잔류분(殘留分)에 관(關)하여 -)

  • Park, Chang-Kyu;Yoo, Jai-Yoon
    • Applied Biological Chemistry
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    • v.15 no.1
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    • pp.7-17
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    • 1972
  • Samples of 13 vegetables were collected, between 14 July and 6 August, 1971, from 15 markets located in 12 different cities and analyzed for Heptachlor residues by gas liquid chromatograph. The residue concentrations of Heptachlor and its epoxide were estimated separately, at a sensitivity level of 0.001 p.p.m., to produce Heptachlor residues on the fresh weight basis. The Heptachlor residues in or on the crops analyzed, including three staple vegetables, potatoe, radish and chinese cabbage, were found fairly low and are far lower than the residue tolerences for respective vegetables recommended jointly by FAO and WHO of the United Nations.

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Alpha-Amylase Immobilization on Epoxy Containing Thiol-Ene Photocurable Materials

  • Cakmakci, Emrah;Danis, Ozkan;Demir, Serap;Mulazim, Yusuf;Kahraman, Memet Vezir
    • Journal of Microbiology and Biotechnology
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    • v.23 no.2
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    • pp.205-210
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    • 2013
  • Thiol-ene polymerization is a versatile tool for several applications. Here we report the preparation of epoxide groups containing thiol-ene photocurable polymeric support and the covalent immobilization of ${\alpha}$-amylase onto these polymeric materials. The morphology of the polymeric support was characterized by scanning electron microscopy (SEM), and energy dispersive spectroscopy (EDS) coupled with SEM was used to explore the chemical composition. The polymeric support and the immobilization of the enzyme were characterized by FTIR analysis. SEM-EDS and FTIR results showed that the enzyme was successfully covalently attached to the polymeric support. The immobilization efficiency and enzyme activity of ${\alpha}$-amylase were examined at various pH (5.0-8.0) and temperature ($30-80^{\circ}C$) values. The storage stability and reusability of immobilized ${\alpha}$-amylase were investigated. The immobilization yield was $276{\pm}1.6$ mg per gram of polymeric support. Enzyme assays demonstrated that the immobilized enzyme exhibited better thermostability than the free one. The storage stability and reusability were improved by the immobilization on this enzyme support. Free enzyme lost its activity completely within 15 days. On the other hand, the immobilized enzyme retained 86.7% of its activity after 30 days. These results confirm that ${\alpha}$-amylase was successfully immobilized and gained a more stable character compared with the free one.

The Effect of Feeding Houttuynia cordata Thunb on Cholesterol and Cholesterol oxides of Pork Lion's (어성초 분말의 혼합 급이가 돈육의 cholesterol 및 산화물에 미치는 영향)

  • Kang, Min-Jung;Joo, Jong-Chan;Shin, Jung-Hye;Choi, Sun-Young;Yang, Seung-Mi;Sung, Nak-Ju
    • Journal of Life Science
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    • v.16 no.6
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    • pp.1029-1035
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    • 2006
  • The study was designed to investigate the influence of feeding Eosungcho(houttutnia cordata Thunb) on the meat quality of porks. Experimental groups were divided into control group(C), 5%(T1) and 10%(T2) Eosungcho powder feeding group, and than administered for 12 weeks. And then pork's loins were storaged at $4^{\circ}C$, for 23 days after vaccum packed. TBARS was increased(P<0.05) during storage days in all samples, while it's contents were lower Eosungcho feding groups than control group. Total cholesterol contents of pork's loin, were $48.9{\pm}0.2\;mg/100\;g$ in control group, $39.1{\pm}0.2\;mg/100\;g$ in T1 group and $37.8{\pm}0.3\;mg/100\;g$ in T2 group. 4 kinds of cholesterol oxides($7{\beta}-hydroxycholesterol$, 19-hydroxycholesterol, ${\alpha}-$ and ${\beta}-epoxide$) detected in pork's loin. Cholesterol oxides concentration of pork's loin was increased during storage and lowest in T2 group.

Clinical Pharmacokinetics of Carbamazepine (Carbamazepine의 임상 약동학)

  • 김민정;류윤미;신완균
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1996.04a
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    • pp.280-280
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    • 1996
  • carbamazepine은 대표적인 항전간제로써, 약물의 유효 혈중 농도 범위가 좁아서 TDM(Theapeutic Drug Monitoring)을 시행하는 약물이다. 그리고 이 약물은 parent drug 뿐만 아니라 대사체의 하나인 carbamazepine-10,11-epoxide 역시 carbamazepine와 동일한 효과가 있는 것으로 알려져 있어, 임상적으로 TDM 시행시에는 carbamazepine의 carbamazepine-10,11-epoxide로의 대사에 소요되는 시간과 대사 정도에 대한 자료가 필요하다. 그러나 이제껏 제시되고 있는 population parameter들이 모두 서양인에 대한 자료이므로 국내에서 이 약물을 투여하는데 있어서 인종간의 차이를 확인하지 않고서 서양인의 자료에 준하여 적용하는 것은 상당한 위험성이 따를 수도 있으므로 한국인에 있어서의 carbamazepine 대사에 관한 연구가 필요하였다. 방법 7명의 건강한 성인을 대상으로 carbamazepine 제제 400mg을 1회 경구 투여한 다음, 0, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72 시간 경과시 채혈하여 정량하였다. 결과 carbamazepine의 AUC 881$\pm$233(minㆍ$\mu\textrm{g}$/$m\ell$), MRT 72.1$\pm$10.8(min), t$_{1}$2/ 40.1 $\pm$ 8.6(min), CL 6.75 $\pm$ 2.72($m\ell$/min/kg), Vdssn 484 $\pm$ 215($m\ell$/kg)의 값을 얻었다.

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Fast, Efficient and Regioselective Conversion of Epoxides to β-Hydroxy Thiocyanates with NH4SCN/Zeolite Molecular Sieve 4 Å under Solvent-Free Conditions

  • Eisavi, Ronak;Zeynizadeh, Behzad;Baradarani, Mohammad Mehdi
    • Bulletin of the Korean Chemical Society
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    • v.32 no.2
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    • pp.630-634
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    • 2011
  • Solvent-free conversion of various epoxides to their corresponding $\beta$-hydroxy thiocyanates was carried out successfully with $NH_4SCN$/zeolite molecular sieve $4{\AA}$ system at room temperature. The reactions were completed within 2 - 7 min to give thiocyanohydrins with perfect regioselectivity and isolated yields. Moreover, the zeolite can be reused for several times without losing its activity.

Design and Synthesis of Novel Epidermal Growth Factor Receptor Kinase Inhibitors

  • Ha, Jae-Du;Kang, Seung-Kyu;Kim, Kun-Do;Choi, Joong-Kwon;Kong, Jae-Yang;Ahn, Chang-H.
    • Bulletin of the Korean Chemical Society
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    • v.26 no.6
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    • pp.959-965
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    • 2005
  • Investigation of structure-activity relationships of novel quinazolines has identified 7,8-dihydro-[1,4]dioxino-[2,3-g]quinazolines as a potent inhibitor of EGFR. These compounds have a benzodioxane framwork, which was prepared by regioselective O-alkylation of ethyl 3,4-dihydroxy benzoate by epoxide ring opening. Compounds 3f and 3k were more potent than ZD-1839 in EGF enzyme and EGFR autophosporylation inhibition assays.

Synthesis of Novel Cyclopropyl Nucleoside Derivatives as Potential Antiherpetic Agent (새로운 사이클로프로필 뉴크레오사이드 유도체의 합성과 생리활성)

  • Kang, Jin-Ah;Chun, Pu-Soon;Moon, Hyung-Ryong
    • YAKHAK HOEJI
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    • v.56 no.4
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    • pp.230-235
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    • 2012
  • Synthesis of novel cyclopropyl pyrimidine and purine nucleoside derivatives 2~8 with ${\alpha}$-configuration was successfully accomplished using an epoxide-ring opening reaction, lactonization, a hydroboration-oxidation reaction and a Mitsunobu reaction as the key steps. Antiviral activities against HSV-1 and -2, HIV-1 and -2, coxsackie B1and B3 viruses and poliovirus were assayed. Three compounds 4, 7 and 8 exhibit cytotoxicity-derived antiviral activity only in HIV-1 and -2.

Synthesis of Cyclic Carbonates under Supercritical Carbon Dioxide (초임계 $CO_2$ 상에서의 고리형 카보네이트의 합성)

  • Yoo, Jin-Yi;Jun, Joon-Ho;Sung, Un-Gyung;Lee, Yoon-Bae
    • Proceedings of the KAIS Fall Conference
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    • 2007.11a
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    • pp.347-349
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    • 2007
  • 지구 온난화를 일으키는 온실 가스 중의 하나인 이산화탄소($CO_2$)를 Epoxide와 Tetrabutylammonium bromide를 촉매로 하여 합성하여, 초임계 $CO_2$ 상태($Tc=31.06^{\circ}C$, Pc=7.38MPa)에서 반응하여 그에 따른 수율을 측정한 결과 초임계하에서는 현저한 수율의 증가를 확인하였다.

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Effect of Cooking and Packaging Methods on the Thiobarbituric Acid Reactive Substances and Cholesterol Oxidation Products of Turkey Thigh Meat Patties During Storage (가열방법과 포장조건이 칠면조육 패티의 저장중 지방산화와 콜레스테롤 산화물에 미치는 효과)

  • Hur, S.J.;Joo, S.T.;Park, G.B.;Kim, I.S.;Jin, S.K.
    • Journal of Animal Science and Technology
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    • v.46 no.3
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    • pp.397-404
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    • 2004
  • Turkey thigh meats with skin were ground twice through a 3-mm plate and patties were prepared. Patties were cooked using 5 different methods(oven cooking, pan frying, oil deep frying, boiling, and microwaving) to an internal temperature of 85${\sim}90^{\circ}C$ and packaged in either oxygen permeable PVC zipperbags or oxygen impermeable PVDC bags. The samples were analyzed for thiobarbituric acid reactive substances(TBARS) and cholesterol oxidation products(COPs) after storage at $4^{\circ}C$. The TBARS of cooked meat increased during the storage regardless of cooking methods, vacuum packaged thigh meat produced less TBARS and COPs than the aerobically packaged samples. At the beginning of storage, aerobically packaged meat cooked by boiling method produced higher TBARS than that of others. However, the TBARS of microwaved meat with vacuum packaging increased rapidly after 3 days of storage at $4^{\circ}C$. The amount of total COPs in cooked thigh meat increased linearly with storage time. The level of total COPs in aerobically packaged cooked meat was higher than the vacuum-packaged meat. Microwave produced higher level of total COPs in meat than other cooking methods during storage.