• Title/Summary/Keyword: One-step synthesis

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Solid-phase Synthesis of 7-Aryl-benzo[b][1,4]oxazin-3(4H)-one Derivatives on a BOMBA Resin Utilizing the Smiles Rearrangement

  • Lee, Ji-Min;Yu, Eun-Ae;Park, Joo-Yeon;Ryu, In-Ae;Shin, Dong-Soo;Gong, Young-Dae
    • Bulletin of the Korean Chemical Society
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    • v.30 no.6
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    • pp.1325-1330
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    • 2009
  • A general method has been developed for the solid phase synthesis of drug-like 7-aryl-benzo[b][1,4]oxazin-3(4H)- one derivatives 6. The method relies on a novel, microwave irradiation promoted cyclization reaction of the BOMBA resin bound, N-substituted-$\alpha$-(2-chloro-4-bromophenoxy)acetamide 3 that takes place via a Smiles rearrangement. The 7-bromobenzo[1,4]oxazine 4, produced in this process is converted to 7-aryloxazin analogs 5 by utilizing Suzuki coupling with various substituted arylboronic acids. Finally, the target 7-aryl-benzo[b][1,4]oxazin-3(4H)-ones 6 are liberated from the resin by treatment with 5% TFA. The progress of the reactions involved in this preparative route can be monitored by using ATR-FTIR spectroscopy on a single bead. The target compounds, obtained by using this five-step sequence, are produced in high yields and purities.

Phosphorylation of Elongation Factor-2 And Activity Of Ca2+/Calmodulin-Dependent Protein Kinase III During The Cell Cycle

  • Suh, Kyong-Hoon
    • BMB Reports
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    • v.33 no.2
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    • pp.103-111
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    • 2000
  • Phosphorylation of the eukaryotic elongation factor 2 (eEF-2) blocks the elongation step of translation and stops overall protein synthesis. Although the overall rate of protein synthesis in mitosis reduces to 20% of that in S phase, it is unclear how the protein translation procedure is regulated during the cell cycle, especially in the stage of peptide elongation. To delineate the regulation of the elongation step through eEF-2 function, the changes in phosphorylation of eEF-2, and in activity of corresponding $Ca^{2+}$/calmodulin (CaM)-dependent protein kinase III (CaMK-III) during the cell cycle of NIH 3T3 cells, were determined. The in vivo level of phosphorylated eEF-2 showed an 80% and 40% increase in the cells arrested at G1 and M, respectively. The activity of CaMK-III also changed in a similar pattern, more than a 2-fold increase when arrested at G1 and M. The activity change of the kinase during one turn of the cell cycle also demonstrated the activation at G1 and M phases. The activity change of cAMP-dependent protein kinase (PKA) was reciprocal to that of CaMK-III. These results indicated: (1) the activity of CaMK-III was cell cycle-dependent and (2) the level of eEF-2 phosphorylation followed the kinase activity change. Therefore, the elongation step of protein synthesis might be cell cycle dependently regulated.

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Optimization of KOGAS DME Process From Demonstration Long-Term Test (KOGAS DME 공정의 실증 시험을 통한 최적화 기술개발)

  • Chung, Jongtae;Cho, Wonjun;Baek, Youngsoon;Lee, Changha
    • Transactions of the Korean hydrogen and new energy society
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    • v.23 no.5
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    • pp.559-571
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    • 2012
  • Dimethyl ether (DME) is a new clean fuel as an environmentally-benign energy resource. DME can be manufactured from various energy sources including natural gas, coal, and biomass. In addition to its environmentally friendly properties, DME has similar characteristics to those of LPG. The aim of this article is to represent the development of new DME process with KOGAS's own technologies. KOGAS has investigated and developed new innovative DME synthesis process from synthesis gas in gaseous phase fixed bed reactor. DME has been traditionally produced by the dehydration of methanol which is produced from syngas, a product of natural gas reforming. This traditional process is thus called the two-step method of preparing DME. However, DME can also be manufactured directly from syngas (single-step). The single-step method needs only one reactor for the synthesis of DME, instead of two for the two-step process. It can also alleviate the thermodynamic limitations associated with the synthesis of methanol, by converting the produced methanol into DME, thereby potentially enhancing the overall conversion of syngas into DME. KOGAS had launched the 10 ton/day DME demonstration plant project in 2004 at Incheon KOGAS LNG terminal. In the mid of 2008, KOGAS had finished the construction of this plant and has successively finished the demonstration plant operation. And since 2008, we have established the basic design of commercial plant which can produce 3,000 ton/day DME.

A New Synthesis of 6,10,14,18-Tetramethyl-5,9,13,17 (E,E,E)-nonadecatetraen-2-one

  • Park, Oee-Sook;Ahn, Su-Kyung
    • Archives of Pharmacal Research
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    • v.16 no.4
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    • pp.265-270
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    • 1993
  • 6, 10, 14, 18-Tetramethyl-5, 9, 131, 17(E, E, E)-nonadecatetraen-2-one was synthesized from geraniol or 6-methyl-5(E)-hepten-2-one in 6 steps, repectively. The key step in both syntheses, was the condensation of phenyl sulfone compound and allylic chloride.

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Reviewing of Integrated Assessment of the Impacts of Climate Change and Sea-Level Rise on Agricultural Sector (기후변화·해수면 상승에 따른 농업부문 통합평가 사례연구 비교분석 및 개선방안)

  • Ahn, SoEun;Oh, SeoYun
    • Journal of Climate Change Research
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    • v.7 no.3
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    • pp.299-314
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    • 2016
  • The aim of this paper is to review integrated assessment studies conducted to address the impacts of climate change sea-level rise on agricultural sector and to derive suggestions for improving the integrated assessment process to assist decision-makers in establishing climate change adaptation policy. We collect integrated assessment studies which are based on the impact-pathway analysis, compare their step-by-step procedures and identify main factors addressed in each step. The assessment process is typically carried out in the sequence of scenario development, determination of assessment scope, physical impact assessment, economic analysis and synthesis of the outcomes from each step. We identify two types of integrated assessment. The first one examines the impacts of changes in temperature and/or precipitation on the crop-cultivation patterns and/or agricultural productivity and resulting economic effects on agricultural sector. The other investigates the impacts of sea-level rise on land use/coverage and resulting economic damages in terms of land-value loss where the effects on agriculture is treated as one sector among others. To enhance integrated assessment, we suggest that 1) scenarios need to incorporate the effects of climate change and sea-level rise simultaneously, 2) scope of the assessment needs to be extended to include ecosystem services as well as crop production, 3) social and cultural aspects need to be considered in addition to economic analysis, and 4) synthesis of the outcomes from each step should be able to combine quantitative as well as qualitative information.

Synthesis and Vibrational Spectroscopic Study of Selectively $3^1-^{18}O$-Labelled Chlorophyll Derivatives

  • Morishita, Hidetada;Tamiaki, Hitoshi
    • Journal of Photoscience
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    • v.9 no.2
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    • pp.356-358
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    • 2002
  • Regioselective 3$^1$-$^{18}$ O-labelling of chlorophyll derivatives possessing a 3-formyl group such as methyl (pyro) pheophorbide-d (3, 4) was carried out efficiently by a simple one-step procedure; by stirring a homogeneous solution of tetrahydrofuran and H$_2$$^{18}$ O containing a small amount of trifuluoroacetic acid.

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Total Synthesis of Norneolignans from Krameria Species

  • Seo , Pil-Ja;Choi, Hong-Dae;Son, Byeng-Wha
    • Archives of Pharmacal Research
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    • v.27 no.12
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    • pp.1189-1193
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    • 2004
  • The total synthesis of norneolignans isolated from Krameria species, 2-aryl-5-(E)-propenylbenzofurans (5, 11), is described. The key step involves the one-pot reaction for 2-arylbenzofurans (2, 7) from 4-hydroxyphenylacetone with 4'-acetoxy-2-chloro-2-(methylthio)acetophenone (1) and 2-chloro-2-methylthio-(2',4',6'-trimethoxy)acetophenone (6) under Friedel-Crafts reactionconditions.

A study on Variable Step Size algorithms for Convergence Speed Improvement of Frequency-Domain Adaptive Filter (주파수영역 적응필터의 수렴속도 향상을 위한 가변스텝사이즈 알고리즘에 관한 연구)

  • 정희준;오신범;이채욱
    • Proceedings of the IEEK Conference
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    • 2000.11d
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    • pp.191-194
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    • 2000
  • Frequency domain adaptive filter is effective to communication fields of many computational requirements. In this paper we propose a new variable step size algorithms which improves the convergence speed and reduces computational complexity for frequency domain adaptive filter. we compared MSE of the proposed algorithms with one of normalized FLMS using computer simulation of adaptive noise canceler based on synthesis speech.

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A Short Synthesis of (Z)-13-Eicosen-10-one the Principal Component of the Peach Fruit Moth Pheromone

  • Lee, Eun;Koh, Soo-Young;Song, Byong-Doo;Park, Tae-Kyo
    • Bulletin of the Korean Chemical Society
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    • v.5 no.6
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    • pp.223-226
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    • 1984
  • (Z)-13-Eicosen-10-one (1), one of the active components of the female pheromone of the peach fruit moth, Carposina niponensis Walsingham, was synthesized from 2-nonanone, succinic anhydride, and n-nonyllithium. The key step involves the preparation of 13-eicosyn-10-one from an epoxyketone via Eschenmoser cleavage.