• 제목/요약/키워드: Sulfones

검색결과 35건 처리시간 0.023초

6-엑소메칠렌 펜남 유도체의 합성 (Synthesis of 6-Exomethylene Penams Derivatives)

  • 임채욱;윤상배;김용현;정미량;임철부
    • 약학회지
    • /
    • 제47권5호
    • /
    • pp.288-292
    • /
    • 2003
  • The synthesis of new 6-exomethylene penams with substituted triazole ring was described. The 6,6-dibromopenam 5 was reacted with $CH_3$MgBr and substituted triazole 4 to afford the 6-bromo penicillanate 6, which was treated with acetic anhydride to give acetoxy compound 7. The deacetobromination of acetoxy compound 7 with zinc and acetic acid gave 6-exomethylene penams 8, which was oxidized to sulfones 9 by m-CPBA. The p-methoxybenzyl compounds 6∼9 were deprotected by AlCl$_3$ and neutralized to give the sodium salts 10∼13.

6-엑소메칠렌 펜남 유도체의 합성 (Synthesis of 6-Exomethylene Penam Derivatives)

  • 임채욱;박희석;이현수;임철부
    • 약학회지
    • /
    • 제44권2호
    • /
    • pp.128-134
    • /
    • 2000
  • The synthesis of new 6-exomethylene penams with triazole ring was described. The 6,6-dibromopenam 5 was treated with $CH_3$MgBr and carbaldehyde 4 to afford the 6-bromo-6-(1-hydroxy-1-methyl)penicillanate 6, which was reacted with acetic anhydride to give acetoxy compound 7. The deacetobromination of 7 with zinc and acetic acid gave 6-exomethylenpenams, Z-isomer 8 and E-isomer 9, which were oxidized to sulfones 10 and 11 by m-CPBA. The p-methoxybenzyl compounds 6~11 were deprotected by AlCl$_3$ and neutralized to give the sodium salts 12~17.

  • PDF

6-트리아졸 엑소메칠렌펜남 유도체의 합성 (Synthesis of 6-Triazole Exomethylenepenams Derivatives)

  • 김연숙;오정석;임채욱;임철부
    • 약학회지
    • /
    • 제48권5호
    • /
    • pp.303-308
    • /
    • 2004
  • The synthesis of new 6-triazole exomethylenepenams was described. The 6,6-dibromopenam 5 was reacted with $CH_3$MgBr and substituted triazole 4 to afford the 6-bromo penicillanate 6, which was treated with acetic anhydride to give acetoxy compound 7. The deacetobromination of acetoxy compound 7 with zinc and acetic acid gave 6-exomethylene penams 8 and 9, which were oxidized to sulfones 10 and 11 by m-CPBA. The p-methoxybenzyl compounds 6-11 were deprotected by AlCl$_3$ and neutralized to give the sodium salts 12-17.

술폰화 poly(arylene ether sulfones) 양이온 교환막의 술폰산기 농도 변화에 따른 특성 (Characteristics of Sulfonated Poly(arylene ether sulfones) Cation-Exchange Membrane by Variation of Sulforic Acid Group Concentration)

  • 김래현;이승용;최선용;이정우;박세용
    • 전기화학회지
    • /
    • 제3권1호
    • /
    • pp.57-62
    • /
    • 2000
  • 이온 교환막의 고정이온 농도변화에 따른 막 특성을 알아보기 위해 matrix인 PSF (polysulfone)과 술폰화제인 CSA(chlorosulfuric acid)의 몰 비를 달리하여 SPSF (sulfonated polysulfone) 양이온 교환수지를 합성하였다. 합성된 SPSF의 이온교환용량, 함수율, 고정이온 농도, 분배계수 등을 측정하였다. DSC, TGA분석으로부터 SPSF의 술폰산기 농도 증가에 따라 벌키한 술폰산기의 도입으로 인하여 유리전이 온도는 증가하고 중량 감소비는 감소하는 것으로 나타났다. 본 실험조건에서는 SPSF막의 구조가 SEM, AFM등의 분석을 통하여 비대칭인 것으로 나타났다. 교류 임피던스로부터 측정한 SPSF 막을 통한 $Na^+$ 이온의 겉보기 확산계수는 술폰산기 농도 증가에 따라 증가하였다.

6-엑소메칠렌 Sulbactam 유도체의 합성 (Synthesis of 6-Exomethylene Sulbactam Derivatives)

  • 임채욱;정홍식;임철부
    • 약학회지
    • /
    • 제46권6호
    • /
    • pp.381-386
    • /
    • 2002
  • The synthesis of new 6-exomethylene sulbactam derivatives with 5-methyl-1,3,4-thiadiazole was described. The 6,6-dibromopenam 5 was reacted with $CH_3$MgBr and carbaldehyde 4 to afford the 6-bromo-6-(1-hydroxy-1-methyl)penicillanate 6, which was treated with acetic anhydride to give acetoxy compound 7. The deacetobromination of acetoxy compound 7 with zinc and acetic acid gave 6-exomethylen penams, Z-isomer 8 and E-isomer 9, which was oxidized to sulfones 10 by m-CPBA. The p-methoxybenzyl compounds 6-10 were deprotected by AlCl$_3$ and neutralized with NaOH solution to give the sodium salts 11-15.

2-and 3-Substituted Cephalosporin Sulfones 유도체의 합성 및 Human Leukocyte Elastase 억제작용에 관한 연구

  • 임채욱;임철부
    • 한국응용약물학회:학술대회논문집
    • /
    • 한국응용약물학회 1994년도 춘계학술대회 and 제3회 신약개발 연구발표회
    • /
    • pp.230-230
    • /
    • 1994
  • Human leukocyte elastase(HLE)는 폐와 피부, 혈관등의 Connective tissue의 주요 구성물인 elastin을 분해하는 효소로써, 백혈구의 식균작용에도 관여한다. 그러나 이효소가 과다하게 분비되면 pulmonary emphysema와 adult respiratory distress syndrome, rheumatoid arthritis를 유발한다고 알려지고 있다. 지금까지 HLE억제제로 시판되는 의약품은 없으나, 최근에 Cephalosporin유도체가 이 효소의 억제제로 우수한 효과가 있다는 보고가 있은 후, HLE억제제로써 이들의 유도체가 개발되고 있다. 연구자들은 다음일반식에서 2번과 3번위치에 치환기를 도입시킨 수종의 Cephalosporin Sulfone의 유도체들을 합성하고. 이들의 HLE억제 효과를 Spectrophotometerqkdtlr을 이용하여 측정하였다. 합성화합물증 몇가지는 우수한 HLE억제효과를 보여주었고, 2번위치에 diphenylcyclopropyl ring과 같은 부피가 큰 치환체를 도입하면 효소억제력이 증가되었다.

  • PDF