Synthesis of benzothiophene analogues of ketoconazole and itraconazole

被引：2

作者：

Bolos, J ^{[1
]}

Gubert, S ^{[1
]}

Anglada, L ^{[1
]}

Sacristan, A ^{[1
]}

Ortiz, JA ^{[1
]}

机构：

[1] Ctr Invest Grp Ferrer, Dept Med Chem, Barcelona 08028, Spain

来源：

JOURNAL OF HETEROCYCLIC CHEMISTRY | 1997年 / 34卷 / 06期

关键词：

D O I：

10.1002/jhet.5570340611

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The synthesis of the benzothiophene analogues of the orally active antifungal agents ketoconazole and itraconazole 3a and 3b is reported. The key heterocyclic system 3-(1-piperazinyl)benzo[b]thiophene is prepared by formation of the enamine between a benzothienone and ethyl 1-piperazinecarboxylate. After elaboration of the respective N-substituents, the methoxy group is cleaved with boron tribromide, and O-alkylated with the corresponding mesylates.

引用

页码：1709 / 1713

页数：5

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