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Journal of the Korean Chemical Society (JKCS)

ISSN 1017-2548(Print)
ISSN 2234-8530(Online)
Volume 43, Number 6
JKCSEZ 43(6)
December 20, 1999 

A Highly Efficient Synthesis of Itraconazole Intermediates and Their Analogues

Itraconazole 중간체의 효율적 합성법과 그 유사체의 합성
Chong Il Ahn, Young Chan Myoung, Ha Young Choi, Seung Jin Kim

안종일, 명영찬, 최하영, 김승진
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 4위치의 methoxy기 대신 2-, 3- 위치에 methoxy기를 가진중간체 화합물을 합성하고 이로부터 Itraconazole 유사체도 합성할 수 있었다.

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-methoxygroup were synthesized.

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