Synthesis of the integrastatin nucleus using the Ramberg-Bilcklund reaction

被引:31
作者
Foot, JS [1 ]
Giblin, GMP
Taylor, RJK
机构
[1] Univ York, Dept Chem, York YO10 5DD, N Yorkshire, England
[2] GlaxoSmithKline, Dept Med Chem Neurol, Welwyn Garden City AL6 9AR, Herts, England
[3] GlaxoSmithKline, GI CEDD, Welwyn Garden City AL6 9AR, Herts, England
关键词
D O I
10.1021/ol035786v
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The first synthesis of the tetracyclic nucleus of the Integrastatins, natural products that have been shown to selectively inhibit HIV-1 integrase, is reported. Key steps of this synthesis involve a novel cis-selective Ramberg-Backlund reaction and an unusual Lewis acid-promoted cyclization step.
引用
收藏
页码:4441 / 4444
页数:4
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