Journal of the Korean Chemical Society (대한화학회지)

Korean Chemical Society (대한화학회)
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A Highly Efficient Synthesis of Itraconazole Intermediates and Their Analogues

Itraconazole 중간체의 효율적 합성법과 그 유사체의 합성

  • Ahn, Chong Il (Department of Chemical Science and Technology, Agency for Technology and Standards, MOCIE) ;
  • Myoung, Young Chan (Department of Chemical Science and Technology, Agency for Technology and Standards, MOCIE) ;
  • Choi, Ha Young (Department of Chemical Science and Technology, Agency for Technology and Standards, MOCIE) ;
  • Kim, Seung Jin (Department of Chemical Science and Technology, Agency for Technology and Standards, MOCIE)
  • 안종일 (산업자원부 기술표준원 유기화학과) ;
  • 명영찬 (산업자원부 기술표준원 유기화학과) ;
  • 최하영 (산업자원부 기술표준원 유기화학과) ;
  • 김승진 (산업자원부 기술표준원 유기화학과)
  • Published : 19991200
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Abstract

Itraconazole is an important drug for oral treatment of histoplasmosis and blastomycosis. ltraconazole has been the targets of many synthetic efforts due to their diverse antifungal activities. ln this study, an efficient synthetic route for Itraconazole intermediates has been developed using new procedures. Also, ltraconazole analogues introducing 2- and 3-methoxy group instead of ltraconazole intermediates with 4-methoxy group were synthesized.

Itraconazole은 다양한 항진균 활성을 가지고 있는 매우 중요한 화합물로써 histoplasmosis, blastomysosis의 경구용 항진균 치료제로 매우 중요하다. 본 연구에서는 Itraconazole 중간체 합성에 있어서 합성과정을 개선하고, 또 ltraconazole 중간체의 4-위치의 methoxy기 대신 2-, 3- 위치에 methoxy기를 가진중간체 화합물을 합성하고 이로부터 Itraconazole 유사체도 합성할 수 있었다.

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References

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