• Title/Summary/Keyword: condensation reaction

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Radiosynthesis of 125I-labeled 2-cyanobenzothiazole: A new prosthetic group for efficient radioiodination reaction

  • Mushtaq, Sajid;Choi, Dae Seong;Jeon, Jongho
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.3 no.1
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    • pp.44-51
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    • 2017
  • Herein we report an efficient radiolabeling method based on a rapid condensation reaction between N-terminal cysteine and 2-cyanobenzothiazole (CBT). Radioiodination of 2-cyano-6-hydroxybenzothiazole 2 was carried out using chloramine-T to give $^{125}I$-labeled CBT ([$^{125}I$]1) with a high radiochemical yield ($90{\pm}6%$ isolated yield, n=3) and radiochemical purity (>99%). To evaluate the radiolabeling efficiency of $^{125}I$-labeled CBT, model compounds, L-cysteine and N-terminal cysteine conjugated cRGD peptide were reacted with [$^{125}I$]1 under mild conditions. The radiolabeling reactions rapidly provided the $^{125}I$-labeled products [$^{125}I$]5 and [$^{125}I$]6 with excellent radiochemical yields and radiochemical purity. Therefore, we demonstrate that [$^{125}I$]1 will be a useful prosthetic group for radioactive iodine labeling of N-terminal cysteine bearing biomolecules.

Preparation of <$\alpha-Fe_2O_3$ fone powders using iron(III) nitrate (철질산염을 이용한 $\alpha-Fe_2O_3$ 미세 분말 제조)

  • 김병수;정용선;오근호
    • Journal of the Korean Crystal Growth and Crystal Technology
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    • v.8 no.1
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    • pp.138-144
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    • 1998
  • $\alpha$-$Fe_2O_3$ fine powders with the sizes smaller than 0.5 $\mu \textrm{m}$ were prepared by the solvolysis and condensation reaction using iron(III) nitrate and ethanol as starting materials. The variation of pH and the change of FT-IR absorption peak were observed to study the reaction mechanism of iron(III) nitrate solution. In addition, the decomposition mechanism of the precipitated gel was investigated by differential scanning calorimeter, X-ray diffractometer and FT-IR spectrometer. Scanning electron microscope and BET method were performed to analyze the effects of Iron (III) nitrate concentration and reaction temperature on the particle size of $\alpha$-$Fe_2O_3$ powders.

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Synthesis of Methyl-substituted Bicyclic Carbanucleoside Analogs as Potential Antiherpetic Agents

  • Kim, Kyung-Ran;Park, Ah-Young;Lee, Hyung-Rock;Kang, Jin-Ah;Kim, Won-Hee;Chun, Pu-Soon;Bae, Jang-Ho;Jeong, Lak-Shin;Moon, Hyung-Ryong
    • Bulletin of the Korean Chemical Society
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    • v.29 no.10
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    • pp.1977-1982
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    • 2008
  • Novel bicyclo[3.1.0]hexanyl purine nucleoside analogues were synthesized as potential antiherpetic agents via a bicyclo[3.1.0]hexanol (${\pm}$)-8, which was prepared using a highly efficient carbenoid cycloaddition reaction. A highly diastereoselective reduction of ketone and a Mitsunobu reaction for the condensation of glycosyl donor (${\pm}$)-12 with 6-chloropurine were employed.

Synthesus of DL-1-Amino Alkyl Phosphonic Acids and Their Derivatives (II) (DL-1-Amino Alkyl Phosphonic Acid 와 그 유도체들의 합성 (ll))

  • Kyung Yeon Cho;Duck Chan Kim;Yong Joon Kim
    • Journal of the Korean Chemical Society
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    • v.15 no.5
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    • pp.275-280
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    • 1971
  • Six previously unreported N-acylated-DL-1-amino alkyl phosphonic acids were prepared; N-Acetyl-DL-1-amino-3-methyl butyl phosphonic acidN-Benzoyl-DL-1-amino-2-methyl propyl phosphonic acidN-Benzoyl-DL-1-amino-3-methyl butyl phosphonic acidN-Benzoyl-DL-1-amino-2-methyl butyl phosphonic acidN-Acetyl-DL-1-amino-2-methyl propyl phosphonic acidN-Acetyl-DL-1-amino-2-methyl butyl phosphonic acidThe first four compounds were characterized, and the last two compounds were obtained in the crude oil state. The above three DL-1-amino-alkyl phosphonic acid were synthesized from iso-valeric acid, iso-caproic acid and ${\beta}$-methyl valeric acid using Hell-Volhard-Zelinsky reaction, the condensation reaction with triethyl-phosphite and the modified Curtius Reaction. Iso-caproic acid and ${\beta$-methyl valeric acid were prepared by the conventional methods.

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Specific Surface Area and Pore Structure Changes of Calcined Lime with Calcination and Sulfation Reaction (소성과 황화반응에 따른 생석회의 비표면적 및 기공구조 변화)

  • 강순국;정명규
    • Journal of environmental and Sanitary engineering
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    • v.13 no.3
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    • pp.19-29
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    • 1998
  • The calcination reactivity of limestone and physical property changes of calcined lime were investigated with a temperature($720~1000^{\circ}C$ under atmospheric gas($N_2$, $CO_2$) conditions. The mechanisms of mass transport in a lime matrix were represented by the evaporation and condensation (${\gamma}=1.7$) at $1000^{\circ}C$ and the volume diffusion (${\gamma}=2.7$) at $800^{\circ}C$, which was obtained by the specific surface area of calcined lime with sintering conditions. Also, the effect of physical property on the reactivity of sulfation reaction was determined by the changes of pore size with $lime-SO_2$ reaction in this work. The initial sulfation rate of calcined lime increased with increasing temperature, whereas the capture capacity of $SO_2$ exhibited a maximum value at $900^{\circ}C$. The pore volume of sulfated lime was decreased with increasing sulfation time, but the major pores shifted to the distribution of larger size at a temperature of $850{\;}~{\;}1000^{\circ}C$. The mean pore size of sulfated lime based on pore volume decreased gradually at $1000^{\circ}C$; however, it increased with sulfation time up to 40 min and rapidly decreased thereafter.

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Effect of Alumina Nanooxide Application on Nitrendipine Manufacturing Process (알루미나 나노산화물이 Nitrendipine 제조 공정에 미치는 영향)

  • Chae, E.J.;Uhm, Y.R.;Han, B.S.;Rhee, C.K.;Park, S.E.
    • Journal of Powder Materials
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    • v.14 no.2 s.61
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    • pp.127-131
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    • 2007
  • The alumina nano powders synthesized by levitational gas condensation (LGC) method were applied to catalyst in manufacturing process of Hanzsch reaction for Nitrendipine. The L-tartaric acid on the surface is carried out with participation of carbonyl fragments, O-H, C-H bonds which affects stereo selectivity, yield on the reagents positively. From the analysis of the IR-spectroscopy, the carbonyl fragments, O-H, and C-H bond were created by the catalytic reaction. From the analysis of the rR-spectroscopy, the carbonyl fragments, O-H, and C-H bond were created by the catalytic reaction. The newly created bonds made a chiral center on the final product.

Preparation of Ferroelectric PZT Thin Film by Sol-Gel Processing; (II) Effect of Catalysts on Densification and Crystallization (솔-젤법에 의한 강유전성 PZT 박막의 제조;(II) 치밀화 및 결정화에 미치는 촉매의 영향)

  • 김병호;박성호;김병호
    • Journal of the Korean Ceramic Society
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    • v.32 no.7
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    • pp.783-792
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    • 1995
  • Sol-Gel derived ferroelectric PZT thin films were fabricated on ITO/Glass and Si/SiO2 substrates. In order to investigate the effect of catalysts on the densification and crystallization of PZT thin films, a nitric acid or ammonium hydroxide was added to the PZT stock solution at the state of partial hydrolysis reaction. The measured pH for a stable PZT sol was 5.2~9.3. In case of an acid-catalyzed PZT sol, a highly condensed particulate PZT sol was formed by accelerating the hydrolysis reaction. But weakly branched polymeric PZT sol was formed with a base-catalyzed condition. The difference in densification behavior was not found in the pH range of added catalyst, but the refractive index of PZT thin film was increased rapidly as the annealing temperature increased. The PZT thin film annealed at 54$0^{\circ}C$ for 10 min was fully densified and its refractive index was above 2.4. When the annealing temperature increased, the transition from the pyrochlore phase to perovskite appeared at 54$0^{\circ}C$. The base-catalyzed PZT thin film suppressed to form the pyrochlore phase and proceeded effectively to convert the perovskite phase. This was due to the formation of polymeric molecular structure by controlling the hydrolysis and condensation reaction through the additiion of the ammonium hydroxide.

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A New Synthetic Studies on Anticancer Agent Methotrexate (Anticancer Agent인 Methotrexate에 대한 새로운 합성 연구)

  • Yu Euy Kyung;Ryu Seoung Ryuall
    • Journal of the Korean Chemical Society
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    • v.37 no.1
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    • pp.136-140
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    • 1993
  • New synthetic method for diethyl N-[4-{[(2,4-diamino-6-yl)methyl]-amino}benzoyl]-L-glutamate(10) which is an intermediate of methotrexate is described. p-Nitrobenzoyl-L-glutamate was obtained via a two-step sequence which involves condensation of p-nitrobenzoyl chloride with diethyl-L-glutamate and Fischer esterification reaction with ethanol. Reductive methylation of diethyl-p-nitrobenzoyl-L-glutamate were carried out by reaction with formic acid and paraformaldehyde in the presence of $PtO_2$ catalyst and yielded diethyl N-(4-methylaminobenzoyl)-L-glutamate(7). It was followed by allylation and iodoazidozation to give the diethyl-p-[N-(2-azido-3-iodopropyl)-N-methyl]aminobenzoyl-L-glutamate(9). The cyclization reaction of compound(9) with 2,4,5,6-tetraaminopyrimidine was carried out by intermolecular nucleophilic substitution to give the desired methotrexate diethylester.

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EXPERIMENTAL STUDY ON THE EFFECT OF RADIATION IN THE SECONDARY PALATE FORMATION. (방사선조사가 구강형성기에 미치는 영향에 관한 실험적 연구)

  • You Dong Soo
    • Journal of Korean Academy of Oral and Maxillofacial Radiology
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    • v.7 no.1
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    • pp.9-15
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    • 1977
  • The author observed the effect of X-ray irradiation on the secondary palate formation of the rat fetuses. The mothers were exposed to X-radiation on the 10½th, 11½th and 12½th day of gestation with respectively 150, 200, 250, 300 and 350 rads. The fetuses were removed from mothers on 15½h, 16½th and 18½th day of gestation. Morphological changes in palate formation were examined and histochemical preparations were made. 1. In control fetuses, the secondary palates were fully developed on the 15½th to 18½th day of gestation. But in experimental fetuses, many cleft palates were observed in accordance with increase of X-radiation dose. 2. Frequency of incidence of horizontal position of both palated shelves in cleft palate was highest. 3. Accordig to the dislocation of palatal processes, the stain ability of palatal crest was varied. 4. The thickened area of palatal epithelium of palatal crest showed intense methyl green-pyronin and PAS reaction 5. Mesenchymal cell condensation was appeared under the thickened epithelium of palatal process and this mesenchymal tissue showed strong colloidal iron reaction. 6. The stain ability of alizarin red S and alkaline phosphatase reaction of tectal ridge were decreased, in accordance with increase of irradiation doses.

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The Synthesis of Vanadium-Doped Forsterite by the $H_2O_2$-Assisted Sol-Gel Method, and the Growth of Single Crystals of Vanadium-Doped Forsterite by the Floating Zone Method

  • 박동곤;Mikio Higuchi;Rudiger Dieckmann;James M. Burlitch
    • Bulletin of the Korean Chemical Society
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    • v.19 no.9
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    • pp.927-933
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    • 1998
  • Polycrystalline powder of vanadium-doped forsterite (Vδ $Mg_2SiO_4$) was synthesized by the $H_2O_2$-assisted sol-gel method. The vanadium dopant, which was added as VO$(OMe)_3$ in methanol, went through several redox reactions as the sol-gel reaction proceeded. Upon adding VO$(OMe)_3$ to a mixture of $Mg(OMe)_2$ and Si$(OEt)_4$ in methanol, V(V) reduced to V(IV). As hydrolysis reaction proceeded, the V(IV) oxidized all back to V(V). Apparently, some of the V(V) reduced to V(IV) during subsequent gelation by condensation reaction. The V(IV) remained even after heat treatment of the gel in highly oxidizing atmosphere. The crystallization of the xerogel around 880 ℃ readily produced single phase forsterite without any minor phase. Using the polycrystalline powder as feeding stock, single crystals of vanadium-doped forsterite were grown by the floating zone method in oxidizing or reducing atmosphere. The doping was limited in low level because of the high partitioning of the vanadium in liquid phase during melting. The greenish single crystal absorbed visible light of 700∼1100 nm. But, no emission was obtained in near infrared range.