Total Synthesis of Desmethyl Macrolide Antibiotics

被引：13

作者：

Andrade, Rodrigo B. ^{[1
]}

机构：

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

来源：

SYNLETT | 2015年 / 26卷 / 16期

基金：

美国国家卫生研究院;

关键词：

total synthesis; desmethyl macrolides; ketolide antibiotics; telithromycin; erythromycin; OLEFIN METATHESIS CATALYSTS; PEPTIDYL TRANSFERASE CENTER; ANTIBACTERIAL ACTIVITY; SECONDARY ALCOHOLS; HIGHLY POTENT; ERYTHROMYCIN; RESISTANT; KETOLIDES; STEREOCHEMISTRY; TELITHROMYCIN;

D O I：

10.1055/s-0034-1381047

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Macrolide antibiotics occupy a special place in the history of organic chemistry and medicine. This account chronicles the evolution of our approach that ultimately led to the successful total syntheses of four desmethyl (i.e., Me -> H) analogues of telithromycin, a semisynthetic derivative of the flagship macrolide antibiotic, erythromycin. 1 Introduction 2 Project Rationale and Retrosynthetic Analysis 3 Lessons Learned from the Total Synthesis of 4,8,10-Tridesmethyl Telithromycin 4 Total Synthesis of 4,10-Didesmethyl Telithromycin 5 Total Synthesis of 4,8-Didesmethyl Telithromycin 6 Total Synthesis of 4-Desmethyl Telithromycin 7 Biological Evaluation of Desmethyl Telithromycin Analogues 8 Concluding Remarks

引用

页码：2199 / 2215

页数：17

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