• 제목/요약/키워드: amination

검색결과 125건 처리시간 0.021초

잠재적 항암작용이 있는 6-Allylthio-3-aminopyridazine 유도체의 합성 (Synthesis of Potential Anticancer 6-Allylthio-3-aminopyridazine Derivatives)

  • 박은희;박명숙
    • 대한화학회지
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    • 제51권3호
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    • pp.244-250
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    • 2007
  • 항암작용이 기대되는 일련의 새로운 6-allylthio-3-aminopyridazine 유도체를 allylthiolation, amination을 이용하여 합성하였다. 피리다진 핵은 hydrazine monohydrate와 maleic anhydride의 축합반응으로 제조하였다. 3,6- Dichloropyridazine은 3,6-dihydroxypyridazine을 POCl3에 가하여 합성하였다. 6-Allythio-3-chloropyridazine은 3,6- dichloropyridazine에 allylmercaptan과 sodium hydroxide을 이용하여 얻었다. Morpholine, piperazine, pyrazole, imidazole, pyrrolidine, piperidine, perhydroazepine 및 perhydroazocine와 같은 질소 친핵체를 갖는 hetero환을 피리 다진 환의 3번 위치에 도입시켜 6-allylthio-3-aminopyridazine 합성하였다. 이 과정은 아민 친핵체의 친핵성 치환반응 으로 n-buthanol에서 NH4Cl를 가하고 24~48시간 동안 환류시켜 진행하였다.

Improving Catalytic Efficiency and Changing Substrate Spectrum for Asymmetric Biocatalytic Reductive Amination

  • Jiang, Wei;Wang, Yali
    • Journal of Microbiology and Biotechnology
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    • 제30권1호
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    • pp.146-154
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    • 2020
  • With the advantages of biocatalytic method, enzymes have been excavated for the synthesis of chiral amino acids by the reductive amination of ketones, offering a promising way of producing pharmaceutical intermediates. In this work, a robust phenylalanine dehydrogenase (PheDH) with wide substrate spectrum and high catalytic efficiency was constructed through rational design and active-site-targeted, site-specific mutagenesis by using the parent enzyme from Bacillus halodurans. Active sites with bonding substrate and amino acid residues surrounding the substrate binding pocket, 49L-50G-51G, 74M,77K, 122G-123T-124D-125M, 275N, 305L and 308V of the PheDH, were identified. Noticeably, the new mutant PheDH (E113D-N276L) showed approximately 6.06-fold increment of kcat/Km in the oxidative deamination and more than 1.58-fold in the reductive amination compared to that of the wide type. Meanwhile, the PheDHs exhibit high capacity of accepting benzylic and aliphatic ketone substrates. The broad specificity, high catalytic efficiency and selectivity, along with excellent thermal stability, render these broad-spectrum enzymes ideal targets for further development with potential diagnostic reagent and pharmaceutical compounds applications.

저농도 이산화탄소 포집용 활성탄소섬유 흡착제의 질소작용기 함침연구 (Impregnation of Nitrogen Functionalities on Activated Carbon Fiber Adsorbents for Low-level CO2 Capture)

  • 황수현;김동우;정동원;조영민
    • 한국대기환경학회지
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    • 제32권2호
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    • pp.176-183
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    • 2016
  • Activated carbon fibers (ACFs) for $CO_2$ adsorption were prepared from polyacrylonitrile (PAN) fiber through the systematic processes such as oxidation, activation and amination with the focus on the formation of nitration functional groups. Textural analysis of test samples revealed the decrease of specific surface area and pore volume by chemical activation including amination. The ratio of micropores to the total volume was 0.85 to 0.91, which was high enough with the pore size of 1.57 to 1.77 nm. Nitrogen compounds such as imine, pyridine and pyrrole presenting favorable interforces to $CO_2$ molecules were formed throughout the whole preparation steps. The aminated ACF adsorbent showed the enhanced adsorption capacity, 0.40 mmol/g for low-level $CO_2$ flow (3000 ppm) at room temperature. Selectivity of $CO_2$ against dry air ($O_2$ & $N_2$) also increased from 1.00 to 4.66 by amination.

Synthesis of Facial Amphiphile 3,7-Diamino-5α-cholestane Derivatives as a Molecular Receptor

  • Ahmad, Md. Wasi;Jung, Young-Mee;Khan, Sharaf Nawaz;Kim, Hong-Seok
    • Bulletin of the Korean Chemical Society
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    • 제30권9호
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    • pp.2101-2106
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    • 2009
  • A series of facial amphiphiles 3,7-diaminocholestane were synthesized from 3,7-diketocholestane via 2 sequential reductive aminations and anion recognition was evaluated with acetate, chloride, bromide, fluoride and phosphate anions. The stereo-selective reductive amination protocol was utilized to synthesized facial amphiphiles afforded receptors in high yields. The molecular receptor 2 showed the highest binding constant with acetate in a 1:1 ratio.

Quaternary Ammonium Polysulfone막의 제조 및 투과 특성 (I) - Quaternary Ammonium Polysulfone의 제조 - (The Preparation of Quaternary Ammonium Polysulfone and its Permeation Behavior (I) -Preparation of Quaternary Ammonium Polysulfone-)

  • 현진호;전종영;김종호;탁태문
    • 멤브레인
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    • 제6권2호
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    • pp.72-78
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    • 1996
  • 양이온성의 quaternary ammonium polysulfone인 AMPS는 2단계 과정을 통하여 제조하였다. 먼저, 폴리술폰을 chloromethyl methyl ether와 촉매로 ZnO를 사용하여 chloromethylation반응으로 CMPS를 제조하는 단계와 준비된 CMPS에 triethylamine을 반응시켜 quaternary ammonium기를 도입시키는 amination 단계로 이루어 진다.

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Compositional Sugar Analysis of Antitumor Polysaccharidees by High Performance Liquid Chromatography and Gas Chromatography

  • Kim, Yeong-Shik;Park, Kyung-Shin;Park, Ho-Koon;Kim, Sung-Whan
    • Archives of Pharmacal Research
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    • 제17권5호
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    • pp.337-342
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    • 1994
  • Carbohydrate analysis is important in studying structure and activity of complex polysaccharides. New analytical method was applied to get an information on the composition of polysaccharides showing antitumor activity. Monosaccharides were labeled with 7-amino-1, 3-naph-thalenedisulfonic acid (7-AGA) by reductive amination and separated by HPLC. Five kinds of polysaccharides from Basidiomycetes were hydrolyzed and analyzed in combination with electrophresis and HPLC. At the same time, alditol acetate derivatives were prepared and analyzed by gas chromatography. Two different techniques using different derivatization methods showed very similar results. The monosaccharides from Coriolus versicolor and Cordyceps militaris were glucose and galactose. Phellinus linteus composed of glucose, glactose, mannose, arabinose and fucose. The HPLC method with fluorescence detector was very sensitive compared to other methods.

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DFT 계산을 이용한 Buchwald-Hartwig amination 반응 메커니즘 연구

  • 강성우
    • EDISON SW 활용 경진대회 논문집
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    • 제3회(2014년)
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    • pp.371-383
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    • 2014
  • 이 연구에서는 팔라듐 착물 $Pd(PPh_3)_2$을 사용한 bromotoluene과 morpholine간의 coupling reaction (Buchwald-Hartwig amination) 반응 메커니즘을 계산화학적 방법을 이용하여 연구하였다. 용매화 자유에너지를 고려한 중간체 에너지를 비교하였으며, 반응물질이 o-bromotoluene 일 때와 p-bromotoluene 일 때, 반응 중간체로 monophosphine 착물이 형성되는 경우와 bisphosphine 착물이 형성되는 경우를 비교하였으며, 반응 중간체로 bisphosphine 착물이 형성되는 경우 cis 이성질체가 중간체인 경우와 trans 이성질체가 중간체인 경우를 비교하였다. 그 결과, 반응물로 p-bromotoluene을 사용할 때 o-bromotoluene을 사용할 때보다 중간체가 상대적으로 더 안정하여 더 좋은 수득률을 얻을 수 있을 것으로 예상되었다. 또한 $Pd(PPh_3)_n(o-tolyl)(N(CH_2CH_2)_2O)$ (n=1 또는 2) 중간체를 제외하고는 모든 경우에서 bisphosphine 중간체가 형성되는 반응경로가 더 안정한 것으로 밝혀졌다. 그리고 $Pd(PPh_3)_2ArBr$의 경우 trans 이성질체가 cis 이성질체보다 안정하지만 $Pd(PPh_3)_2Ar(N(CH_2CH_2)_2O)$의 경우 반대로 cis 이성질체가 trans 이성질체보다 안정한 것으로 나타났다.

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