Total Synthesis of (-)-4,8,10-Tridesmethyl Telithromycin

被引：26

作者：

Velvadapu, Venkata ^{[1
]}

Paul, Tapas ^{[1
]}

Wagh, Bharat ^{[1
]}

Glassford, Ian ^{[1
]}

DeBrosse, Charles ^{[1
]}

Andrade, Rodrigo B. ^{[1
]}

机构：

[1] Temple Univ, Dept Chem, Philadelphia, PA 19122 USA

来源：

JOURNAL OF ORGANIC CHEMISTRY | 2011年 / 76卷 / 18期

关键词：

SECONDARY ALCOHOLS; ERYTHROMYCIN; ANTIBIOTICS;

D O I：

10.1021/jo201319b

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Novel sources of antibiotics are required to address the serious problem of antibiotic resistance. Telithromycin (2) is a third-generation macrolide antibiotic prepared from erythromycin (1) and used clinically since 2004. Herein we report the details of our efforts that ultimately led to the total synthesis of (-)-4,8,10-tridesmethyl telithromycin (3) wherein methyl groups have been replaced with hydrogens. The synthesis of desmethyl macrolides has emerged as a novel strategy for preparing bioactive antibiotics.

引用

页码：7516 / 7527

页数：12

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