• Title/Summary/Keyword: Three component reactions

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Photo- and Sonic Degradation of Endosulfans(α, β, and sulfate) in Aqueous Solution (엔도설판류의 광 및 초음파분해)

  • Kwon, Sung Hyun;Kim, Jong Hyang;Cho, Daechul
    • Korean Chemical Engineering Research
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    • v.45 no.5
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    • pp.460-465
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    • 2007
  • Endosulfan-${\alpha}$ endosulfan-${\beta}$ and endosulfan-sulfate, which are classified as pesticides, were degraded by use of UV energy and ultrasonic irradiation. The degradation residuals were analysed by gas chromatography with an electron capture detector and TOC (total oragnic carbon) analysis. The reactions were conducted in a quartz annular reactor equipped with a low pressure mercury multilamp (8Wx2) and a sonic generator. All the aqueous solutions were concentrated as 10 mg/L initially. Endosulfans were degraded each to result in 48.2% (${\alpha}$), 50.0% (${\beta}$) and 76.5% (sulfate) of removal efficiency by UV energy, and 66.9% (${\alpha}$), 55.8% (${\beta}$) and 72.7% (sulfate) by ultrasonic irradiation, respectively. In contrast to the results of the single-component solutions, degradation of the endosulfan-sulfate was greatly suppressed to result in the lowest degradation rate and removal efficiency in the three-component solutions. This finding suggests that there should be a reversible reaction with a substantially low equilibrium constant between endosulfan-${\alpha}$ or -${\beta}$ and -sulfate in the coexistence of the three endosulfans. TOC data showed the endosulfans were decomposed by 20%~40% toward complete mineralization, producing a quantity of intermediates induced by the radical reactions. We found that all the decay reactions considered in this study nicely fell into pseudo first-order rate.

A Facile Solvent and Catalyst Free Synthesis of New Dihydro Pyrimidinones as Antimicrobial Agents

  • Hegde, Hemant;Ahn, Chuljin;Gaonkar, Santosh L.;Shetty, Nitinkumar S.
    • Journal of the Korean Chemical Society
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    • v.63 no.6
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    • pp.435-439
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    • 2019
  • An efficient one pot multicomponent synthesis of pyrimidinone derivatives of Biginelli type is described. 4-amino-6-aryl-pyrimidine-5-carbonitrile molecules were synthesized efficiently via three-component Biginelli-type condensation of aldehyde, malononitrile, and semicarbazone as urea substituent in the presence of a catalytic amount of PEG-400 as green medium under microwave irradiation. The reactions proceeded efficiently in the presence of microwave radiation to afford the desired products in good to excellent yields. Products have been confirmed by IR, and NMR spectral analysis. All the molecules were tested for their antimicrobial activity against E. coli, S. aureus, P. aeruginosa and C. tropicalis. Some of the compounds have shown moderate to good inhibition efficiency against both gram-positive and gram-negative bacteria. The potent activity was observed against the fungal species with minimum inhibition concentration 12.5 ㎍/mL.

Design of floating Slab according to Dynamic Load (동하중을 고려한 플로팅궤도 슬래브 설계)

  • Park, Sung-Jae;Ma, Chang-Nam;Park, Myung-Gyun;Lee, Du-Hwa;Jo, Su-Ik
    • Proceedings of the KSR Conference
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    • 2010.06a
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    • pp.268-272
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    • 2010
  • Recently the construction of railway sections passing the central area of cities and stations under railway lines are increasing, and then it is urgently required to take the countermeasures against the railway vibration and the second-phase noise radiated from it. The most efficient countermeasure, out of technologies developed up to now, is the floating slab track which is the track system isolated from the sub-structure by springs. In other countries, the source technologies for anti-vibration design and vibration isolator - one of key components - have been developed and many installation experiences have been accumulated. However, in Korea, since the system design technology and technologies for key components are not yet developed, the foreign system are being introduced without any adjustment, and the key component, vibration isolator, depends on imports. In this study, floating slab was divided into three spans, $k_{dynamic}$ use by examining reactions and member forces was to ensure safety.

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An Efficient Synthesis of 2,4,5-Triaryl-1H-Imidazole Derivatives Catalyzed by Boric Acid in Aqueous Media Under Ultrasound-Irradiation

  • Shelke, Kiran F.;Sapkal, Suryakant;Sonal, Swapnil;Madje, Balaji R.;Shingate, Bapurao B.;Shingare, Murlidhar S.
    • Bulletin of the Korean Chemical Society
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    • v.30 no.5
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    • pp.1057-1060
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    • 2009
  • Boric acid ($BO_3H_3$) is an inexpensive, efficient and mild catalyst for the synthesis of 2,4,5-triaryl-1H-imidazoles in excellent yields from the one-pot three-component condensation of benzil/benzoin, an aldehydes and ammonium acetate in aqueous media under ultrasound at room temperature. The remarkable advantages offered by this method are green catalyst, mild reaction conditions, simple procedures, much faster reactions and excellent yield of products.

1-Benzyl-3-Methyl Imidazolium Hydrogen Sulphate [bnmim][HSO4] Promoted Synthesis of α-Aminophosphonates

  • Sadaphal, Sandip A.;Sonar, Swapnil S.;Kategaonkar, Amol H.;Shingare, Murlidhar S.
    • Bulletin of the Korean Chemical Society
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    • v.30 no.5
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    • pp.1054-1056
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    • 2009
  • We have demonstrated a one-pot three component coupling of an aldehydes, an amines, and triethyl phosphite using 1-benzyl-3-methyl imidazolium hydrogen sulphate [bnmim][][$HSO_{4}$] as an efficient catalyst. All the reactions proceed under solvent-free conditions at room temperature. This methodology afforded the corresponding $\alpha$-aminophosphonates in shorter reaction times with excellent yields.

Laboratory Experiment: Synthesis and Characterization of 4-Methyl-N-(phenylacetyl)benzenesulfonamide through Cu(I)-Catalysis

  • Jung, Byunghyuck
    • Journal of the Korean Chemical Society
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    • v.62 no.3
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    • pp.187-190
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    • 2018
  • A three-component coupling reaction of phenylacetylene, p-toluenesulfonyl azide, and water through copper catalysis is described to provide knowledge of spectroscopy and catalytic reactions and to introduce current research topics in organic chemistry for second-year undergraduate students. In the presence of stoichiometric amounts of phenylacetylene, p-toluenesulfonyl azide, and triethylamine, the reaction was performed with 4 mol% CuCl in water as the sole solvent and was completed in 1.5 h. A practical purification method and recrystallization of the crude reaction mixture resulted in the rapid isolation of the desired product with yields of 42~65%. Students characterized 4-methyl-N-(phenylacetyl)benzenesulfonamide by using melting-point determination, infrared spectroscopy, and nuclear magnetic resonance (NMR) spectroscopy. This experimental procedure and spectroscopic data analysis will serve as a platform for students to apply classroom knowledge in practical state-of-the-art research.

Characterization of the in vitro Activities of the P1 and Helper Component Proteases of Soybean mosaic virus Strain G2 and Tobacco vein mottling virus

  • Lim, Hyoun-Sub;Jang, Chan-Yong;Nam, Ji-Ryun;Li, Meijia;Hong, Jin-Sung;Bae, Han-Hong;Ju, Ho-Jong;Kim, Hong-Gi;Ford, Richard E.;Domier, Leslie L.
    • The Plant Pathology Journal
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    • v.28 no.2
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    • pp.197-201
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    • 2012
  • Potyviruses express their RNA genomes through the production of polyproteins that are processed in host cells by three virus-encoded proteases. Soybean plants produce large amounts of protease inhibitors during seed development and in response to wounding that could affect the activities of these proteases. The in vitro activities of two of the proteases of Soybean mosaic virus (SMV) and Tobacco vein mottling virus (TVMV) were compared in the rabbit reticulocyte lysate in vitro translation system using synthetic RNA transcripts. Transcripts produced from SMV and TVMV cDNAs that included the P1 and helper component-protease (HC-Pro) coding regions directed synthesis of protein products that were only partially processed. Unprocessed poly-proteins were not detected from transcripts that included all of the P1, HC-Pro, P3 and portions of the cylindrical inclusion protein coding regions of either virus. Addition of soybean trypsin inhibitor to in vitro translation reactions increased the accumulation of the unprocessed polyprotein from TVMV transcripts, but did not alter the patterns of proteins produced from SMV. These experiments suggest that SMV-and TVMV-encoded proteases are differentially sensitive to protease inhibitors.

The immunogenicity and safety of three-component DTaP vaccine in Korean infants (우리나라 영아에서 3가 정제 백일해 항원 DTaP 백신의 면역원성 및 안전성)

  • Kang, Jin Han;Kim, Jong Hyun;Lee, Jung Hyun;Lee, Soo Young;Hong, Young Jin;Kim, Chang Hwi
    • Clinical and Experimental Pediatrics
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    • v.50 no.4
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    • pp.355-362
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    • 2007
  • Purpose : We conducted the study to evaluate the immunogenicity and safety of three component DTaP vaccine ($Infanrix^{(R)}$) in a group of Korean healthy infants on a three-dose primary vaccination. And we compared the immunogenicity of this DTaP vaccine with two component DTaP vaccine which has been widely used in Korea. Methods : We enrolled one hundred fifty one healthy infants aged 8-9 weeks. These infants were vaccinated at age 2, 4 and 6 months of age with three component DTaP vaccine. Solicited adverse events were actively monitored for 72 hours following each vaccination, and all adverse events after each vaccination were observed for three weeks. Anti-diphtheria toxoid Ab., anti-tetanus toxoid Ab., anti-pertussis toxin Ab., anti-filamentous hemagglutinin Ab., and anti-pertactin Ab. were measured using ELISA for assessing immunogenicity of study vaccine in 60 infants. Immunogenicity analysis of two component DTaP vaccine was performed with same methods in 14 infants as control. Results : The seroconversion rates of anti-diphtheria toxoid Ab, anti-tetanus toxoid Ab. anti-filamentous hemagglutinin Ab. were 100% in both group. Seroconversion rate of anti-pertactin Ab in study group was 100%, but the rate in control group was 50%. However, geometric mean concentration of anti-pertussis toxin Ab. was higher in control group. Mild local and systemic reactions were observed within three days after vaccination, and no serious adverse events related study vaccine were happened during study period. Conclusion : Our study results suggest that three component DTaP vaccine ($Infanrix^{(R)}$) is a well-tolerable and high immunogenic vaccine, especially anti-Pertactin Ab. of the study vaccine is very immunogenic. It can be available as routine DTaP vaccination in our infants.

Signal Detection for Adverse Events of Finasteride Using Korea Adverse Event Reporting System (KAERS) Database (의약품이상사례보고시스템 데이터베이스를 이용한 피나스테리드의 약물유해반응 실마리 정보 탐색)

  • Baek, Ji-Won;Yang, Bo Ram;Choi, Subin;Shin, Kwang-Hee
    • Korean Journal of Clinical Pharmacy
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    • v.31 no.4
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    • pp.324-331
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    • 2021
  • To investigate signals of adverse drug reactions of finasteride by using the Korea Adverse Events Reporting System (KAERS) database. This pharmacovigilance was based on the database of the drug-related adverse reactions reported spontaneously to the KAERS from 2013 to 2017. This study was conducted by disproportionality analysis. Data mining analysis was performed to detect signals of finasteride. The signal was defined by three criteria as proportional reporting ratio (PRR), reporting odds ratio (ROR), and information component (IC). The signals of finasteride were compared with those of the other drugs; dutasteride (similar mechanism of action), minoxidil (different mechanism but similar indications for alopecia), silodosin (different mechanism but similar indications for BPH). It was examined whether the detected signals exist in drug labels in Korea. The total number of adverse event-drug pairs was reported 2,665,429 from 2013 to 2017, of which 1,426 were associated with finasteride. The number of investigated signals of finasteride was 42. The signals that did not include in the drug label were 29 signals, including mouth dry, hypotension, dysuria etc. The signal of finasteride was similar to that of dutasteride and silodosin but was different to that of minoxidil. Early detection of signals through pharmacovigilance is important to patient safety. We investigated 29 signals of finasteride that do not exist in drug labels in Korea. Further pharmacoepidemiological studies should be needed to evaluate the signal causality with finasteride.

Signal Detection of Alpha-adrenoceptor Antagonist using the KIDS-KAERS database (KIDS-KD) (한국 의약품부작용보고원시자료를 활용한 알파차단제의 이상사례 실마리정보 비교 분석)

  • Hyunji Koo;Jun Young Kwon;Jae-Hyuk Choi;Seung Hun You;Sewon Park;Kyeong Hye Jeong;Sun-Young Jung
    • Korean Journal of Clinical Pharmacy
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    • v.33 no.2
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    • pp.86-96
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    • 2023
  • Background: Using KIDS-KAERS database (KIDS-KD) from 2016 to 2020, the aim is to investigate signals of adverse events of alpha-adrenoceptor antagonists and to present adverse events that are not included in the precautions for use when marketing approval. Methods: This study was conducted by disproportionality analysis. Data mining analysis was performed to detect signals of alpha-adrenoceptor antagonists, such as terazosin, doxazosin, alfuzosin, silodosin, and tamsulosin. The signal was defined by three criteria as proportional reporting ratio (PRR), reporting odds ratio (ROR), and information component (IC). Detected signals were compared with product labeling and the European Medicines Agency-Important Medical Events list. Results: Out of the total number of 408,077 reports for adverse events, 6,750 cases were reported as adverse events of alpha-adrenoceptor antagonists. Dizziness, mouth dryness, hypotension postural, and oedema peripheral are identified as common adverse events of five alpha-adrenoceptor antagonists and are typically listed on drug labels. However, new signals were detected for pneumonia, chronic obstructive airway disease, eye diseases such as glaucoma and cataracts, fracture, and ileus of tamsulosin that were not previously listed on the drug labels in Korea. Conclusions: This study identified signals related to adverse drug reactions of alpha-adrenoceptor antagonists and presented serious adverse events, suggesting new adverse reactions to be aware of when using alpha-adrenoceptor antagonists.