Total synthesis and reassessment of the phosphatase-inhibitory activity of the antitumor agent TMC-69-6H

被引：41

作者：

Fürstner, A

Feyen, F

Prinz, H

Waldmann, H

机构：

[1] Max Planck Inst Kohlenforsch, D-45470 Mulheim, Germany

[2] Max Planck Inst Mol Physiol, D-44227 Dortmund, Germany

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2003年 / 42卷 / 43期

关键词：

heterocycles; natural products; palladium; phosphatases; structure-activity relationships;

D O I：

10.1002/anie.200352268

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

The unexpected selectivity proflie of I (17R)-and (17S)-TMC-69-6H (see formula) suggests that N-hydroxypyridone derivatives constitute a promising new lead structure in the search for selective phosphatase inhibitors. An unprecedented Pd-catalyzed C-C bond formation to a pyranone derivative was a key step in the synthesis of enantiopure (17R)-and (17S)-TMC-69-6H.

引用

收藏

页码：5361 / 5364

页数：4

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