• 제목/요약/키워드: Fluoro

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새로운 Quinolone 항균제 개발 연구

  • 함원훈
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1993년도 제2회 신약개발 연구발표회 초록집
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    • pp.118-118
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    • 1993
  • 퀴놀론 모핵의 합성은 기존에 알려진 합성 방법인 Could-Jacobs방법과 Bayer방법에 의해서 Intermediate로 사용된 7-chloro-1-ethyl-6-fluoro-1, 4-dihydro-4-oxoquinoline-3-carboxylic acid와 1-cyclopropyl-7-chloro-6-Fluoro-1,4-dihydro-4-oxoquinolne-3-carboxylic acid를 합성하였다. Heteroaromatic tin compound는 furan, thiophene, 3-bromopyridine, 2-fluoropyridine에 n-BuLi을 사용하여 metallation 한후 electrophile로 tributyltin chloride를 사용하여 2-tributylstannofuran, 2-tributylst-annothiophene, 3-tributylstannopyridine, 2- fluoro-2-tributylstannop-yridine을 합성할 수 있었다. 이상의 Intermediate와 tin compounds를 p-alladium 촉매하에서 반응시켜 1-ethyl-7-(2-furanyl)-6-fluoro-1,4-dihy-dro-4-oxo-3-quinoline-carboxylic acid (compound 3), 1-ethyl-7-(2-th-iophenyl)-6-fluoro-1,4-dihydro-4-oxo-3-quinol in carboxylic acid(compound 5), 1-ethyl-7-(3-pyridinyl)-6-fluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acid (compound 7), 1-ethyl-7-(2-fluoro-3-pyrid-nyl)-6-fluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acid (compound 9), 1-cyclopropyl-7-(2-furanyl) -6-fluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acid (compound 4), 1-cyclopropyl-7-(2-thiophenyl)-6-fluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acid (compound 6) ,1-cyclopropyl-7-(3-pyridinyl)-6-fluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acid (compound 8), 1-cyclopropyl-7-(2-fluoro-3-pyridinyl)-6-fluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acid (compound 10)를 합성하였다.

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6-Fluoroquinolone Carboxamidopenicillin 유도체의 합성 (The Synthesis of 6-Fluoroquinolone Carboxamidopenicillin Derivatives)

  • 임철부;김정주
    • 약학회지
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    • 제31권2호
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    • pp.92-97
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    • 1987
  • The N-[1H-6-fluoro-1,4-dihydro-4-oxo-7-chloroquinoline-3-carboxy] succinimide was reacted with amoxicillin, ampicillin and 6-APA to give 6-[D-(-)-$\alpha$-{1H-6-fluoro-1,4-dihydro-4-oxo-7-chloroguinoline-3-carboxamido} p-hydroxyphanyl acetamido] penicillanic acid [1], 6-[D-(-)-$\alpha$-{1H-6-fluoro-1,4-dihydro-4-oxo-7-chloroquinoline-3-carboxamido} phenylacetamido] penicillanic acid [10] and 6-[1H-6-fluoro-1,4-dihydro-4-oxo-7-chloroquinoline-3-carboxamido] penicillanic acid [19]. The 1-alkyl-6-fluoro-1,4-dihydro-4-oxo-7-substituted quinoline-3-carboxylic acids were reacted with ethyl chloroformate for making mixed anhydride; these mixed anhydrides were reacted with amoxicillin, ampilcillin and 6-APA to give 6-[D-(-)-$\alpha$-{1-alkyl-6-fluoro-1,4-dihydro-4-oxo-7-substituted quinoline-3-carboxamido} p-hydroxyphenylacetamido] penicillanic acid [2-9], 6-[D-(1)-$\alpha$-{1-alkyl-6-fluoro-1,4-dihydro-4-oxo-7-substituted quinoline-3-carboxamido} phenylacetamidod penicillanic acid [11-18] and 6-[1-alkyl-6-fluoro-1,4-dihydro-4-oxo-7-substituted quinoline-3-carboxamido] penicillanic acid [20-27].

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5-할로겐 치환된 Uracil의 4-Thiosugar Nucleosides의 합성에 관한 연구 (제2보). 5-Fluoro-4'-thiouridine과 5-Chloro-4'-thiouridine의 합성 (Synthesis of 1-(4-Thio-${\alpha},{\beta}$-D-ribofuranosyl)-5-halogenouracils (II). 5-Fluoro-4'-thiouridine and 5-Chloro-4'-thio-uridine)

  • 김정균;조원제;보벡크;윗슬러
    • 대한화학회지
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    • 제19권6호
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    • pp.438-442
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    • 1975
  • Unusual pyrimidine nucleoside인 5-fluoro-4'-thiouridine과 5-Chloro-4'-thiouridine을 5-fluoro-와 5-chlorouracil의 2,4-bis(trimethylsilyl) 유도체들을 만든후, 축합반응하여 합성하였다. Leukemia 1210 cell과 Streptococcus faecium에 대한 기초 생물화학적인 예비시험에 의하면 5-fluoro-4'-thiouridine은 5-fluorouridine보다 억제효과가 월등하여 항암제로서의 전망여하는 앞으로의 임상 화학적인 결과로 구명될것 이라고 예상된다.

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2-Deoxy-2-fluoro-D-arabinofuranose류의 합성 연구 (Synthesis of 2-Deoxy-2-fluoro-D-arabinofuranose Derivatives)

  • 천문우;김문환;김득준;정원근
    • 약학회지
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    • 제28권3호
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    • pp.191-195
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    • 1984
  • A ten-step synthesis of 1, 3-di-O-acetyl-5-O-benzoyl-2-deoxy-2-fluoro-D-arabino-furanose, a versatile intermediate in the synthesis of chemotherapeutically important nucleosides, was achieved from D-glucose. This procedure affords good overall yields of products and is suitable for large scale preparations.

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Vibronic Spectroscopy of Jet-Cooled Benzyl-type Radicals Produced from 2-Fluoro-4-Chlorotoluene by Corona Discharge

  • Chae, Sang Youl;Yoon, Young Wook;Lee, Sang Kuk
    • Bulletin of the Korean Chemical Society
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    • 제34권12호
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    • pp.3565-3569
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    • 2013
  • A home-made pinhole-type glass nozzle was employed to generate vibronically excited but jet-cooled benzyl-type radicals from precursor 2-fluoro-4-chlorotoluene with a large amount of carrier gas He, from which the visible vibronic emission spectrum was recorded with a long-path monochromator. From an analysis of the spectrum observed, it was found that two benzyl-type radicals, 2-fluorobenzyl and 2-fluoro-4-chlorobenzyl radicals, were formed from the precursor in corona discharge. The possible pathway for the production of benzyl-type radicals that can explain the spectroscopic observation is herein proposed. In addition, the electronic energy of the $D_1{\rightarrow}D_0$ transition and the vibrational mode frequencies in the $D_0$ state of the 2-fluoro-4-chlorobenzyl radical were determined for the first time.

3-Chloro-2-(4-chloro-2-fluoro-5-hydroxyphenyl)-4,5,6,7-tetrahydro-2H-indazole의 제조방법에 관한 연구 (New method for the synthesis of 3-chloro-2-(4-chloro-2-fluoro-5-hydroxyphenyl)-4,5,6,7-tetrahydro-2H-indazole)

  • 박창민;박관용;김형래;송종환;황인택;전동주
    • 농약과학회지
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    • 제9권1호
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    • pp.23-25
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    • 2005
  • Protox 저해제인 cyclic imide type 화합물 중에서 EK 5439와 S-275 같은 화합물들의 필수 중간체인 3-chloro-2-(4-chloro-2-fluoro-5-hydroxyphenyl)-4,5,6,7-tetrahydro-2H-indazole은 2-(2-fluoro-4-chloro-5-hydroxyphenyl)-2,3a,4,5,6,7-hexahyoindazol-3-one을 포스겐과 반응시켜서 얻을 수 있다고 알려져 있으나, 수율이 매우 낮고 재현성이 없다. 따라서 이 반응의 부산물들을 분리 확인하여, 이 부산물들이 반응물과 목적물의 이량체임을 밝히고, 이들을 가수분해함으로서 목적물의 합성수율을 높이고 반응물을 거의 대부분 회수할 수 있는 효과적인 방법을 개발하였다.

5'-Fluoro-orotic acid를 이용한 여름느타리버섯의 pyrimidine 영양요구성 균주의 positive 선발 (A Positive Selection for Pyrimidine Auxotrophic Mutants from Basidiospores of Pleurotus sajor-caju Using 5'-Fluoro-orotic acid)

  • 김범기;박수철;정미정;유영복;류진창;권석태
    • 한국균학회지
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    • 제25권1호통권80호
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    • pp.26-29
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    • 1997
  • 여름느타리버섯의 담자포자에 자외선을 조사하여 5'-fluoro-orotic acid(FOA) 선발배지에서 pyrimidine 영양요구성 균주를 직접 선발하였다. 24개의 5'-FOA 저항성 균주중 13개의 pyrimidine 영양요구성 균주를 선발할 수 있었으며, 이들의 mating type group과 성장속도를 측정하여 형질전환을 위한 최적의 DNA수용체를 선발할 수 있었다.

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Synthesis and Luminescent Properties of Tetrafluorophenyl Containing Poly(p-phenylenevinylene) Derivatives

  • Ahn, Taek
    • Transactions on Electrical and Electronic Materials
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    • 제16권3호
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    • pp.162-167
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    • 2015
  • To investigate the effect of fluoro groups substitution on poly(p-phenylenevinylene) derivatives, poly(2,3,5,6- tetrafluoro-p-phenylenevinylene-alt-N-ethylhexyl-3,6-carbazolevinylene), PCTF-PPV, and poly[2,3,5,6-tetrafluoro-p-phenylenevinylene-alt-2-methoxy-5-(2-ethylhexyloxy)-p-phenylenevinylene], PMTF-PPV, were synthesized by the well-known Wittig condensation polymerization process. To compare the influences of fluoro groups, no fluoro groups containing model polymers, poly(p-phenylenevinylene-alt-N-ethylhexyl-3,6-carbazolevinylene), PCPPPV and poly[p-phenylenevinylene-alt-2-methoxy-5-(2-ethylhexyloxy)-p-phenylenevinylene], p-PMEH-PPV, were also synthesized. The resulting polymers were completely soluble in common organic solvents and exhibited good thermal stability up to 300℃. The polymers showed UV-visible absorbance and photoluminescence (PL) in the ranges of 259~452 nm and 500~580 nm, respectively. The tetrafluorophenyl containing PCTF-PPV and PMTF-PPV showed relatively red-shifted PL peaks at 521 nm and 580 nm, respectively, compared to that of non-fluoro groups containing polymers (PCP-PPV: 500 nm and p-PMEH-PPV: 539 nm). The single-layer light-emitting diode was fabricated in a configuration of ITO/polymer/Al. Electroluminescene (EL) emissions of PCP-PPV, PCTF-PPV, p-PMEH-PPV and PMTF-PPV were shown at 507, 524, 556, and 616 nm, respectively.

A Study on the Fluoro-polymer Composite Coatings for Protecting the Corrosion of Fossil-fuel Power Plants

  • Kang, Min Soo;Lee, Byung Seung;Chang, Hyun Young;Jin, Tae Eun;So, Il Soo
    • Corrosion Science and Technology
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    • 제6권2호
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    • pp.62-67
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    • 2007
  • Several heavy duty coatings at an every kind industry facilities to various systems currently have been applied review to the many industry fields. Corrosion-protective characteristics in the case of novolac epoxy among them and unsaturated polyester have been applied most widely. epoxy and flake heavy duty coatings are applied for such reason in an every kind facilities(stack, FGD, cooler, chemical tank etc) of a fossil-fuel power plants Cases of the fossil-fuel power plants are exposed to more severe corrosion environment compared with other facilities and It is difficult to display the performance of long-term method at apply to be the partial. Our study shows fluoro-polymer composite coating method to overcome of the limit. The comparison did previous method and heavy duty coating about FGD plants most at a corrosion environment among fossil-fuel power plants. Additionally, other facilities examined different heavy duty method. The design mode of fluoro-polymer composite coating according to an every kind facilities show extensive methods that are characteristic revelation of film(top, middle and primer layer) composition of the paint, film thickness in accordance with a facilities corrosion and the corrosion protective effectiveness to come into being use fluoro-polymer composite with heavy duty paint(epoxy).

Fluoro-quinolone Carboxylic Acid 유도체로부터 탄소-불소 및 수소-불소간 Coupling Consstants의 조사 (Survey of Carbon- and Proton-Fluorine Coupling Constants in Fluoro-quinolone Carboxylic Acid Derivatives)

  • 고동수;이인원;임융호
    • Applied Biological Chemistry
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    • 제41권7호
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    • pp.550-555
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    • 1998
  • Fluoro-quinolone carboxilic acid 유도체에서, 탄소-불소간 one bond coupling constants는 위치와 무관하게 249 Hz에서 257 Hz 사이의 값을 갖는데, geminal 및 vicinal coupling constants는 위치에 따라 그 값의 차이가 많이 생긴다. 즉, seminal coupling constants는 6 Hz에서 23 Hz의 값을 보이고 vicinal coupling constants는 1.9 Hz에서 7 Hz의 값을 보인다. 또한 수소-불소간 three bond coupling constants는 9 Hz에서 10.3 Hz의 값을 보이고, four bond coupling constants는 6 Hz에서 8.3 Hz의 값을 보인다.

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