Synthetic Studies on Et-743. Assembly of the Pentacyclic Core and a Formal Total Synthesis

被引：53

作者：

Fishlock, Dan ^{[1
]}

Willlams, Robert M. ^{[1
,2
]}

机构：

[1] Colorado State Univ, Dept Chem, Ft Collins, CO 80523 USA

[2] Univ Colorado, Ctr Canc, Aurora, CO 80045 USA

来源：

JOURNAL OF ORGANIC CHEMISTRY | 2008年 / 73卷 / 24期

基金：

美国国家卫生研究院;

关键词：

D O I：

10.1021/jo801159k

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A formal total synthesis of the potent anticancer agent Et-743 is described. The tetrahydroisoquinoline core is stereoselectively constructed using a novel radical cyclization of a glyoxalimine. Further elaboration of this core rapidly accessed the pentacyclic core of Et-743. but a mixture of regiosisomers was obtained in the key Pictet-Spengler ring closure. A known advanced intermediate in the synthesis of Et-743 was intercepted, constituting a formal synthesis of the molecule.

引用

页码：9594 / 9600

页数：7

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