Rapid entry into the cryptophycin core via an acyl-β-lactam macrolactonization:: Total synthesis of cryptophycin-24

被引：41

作者：

Eggen, MJ ^{[1
]}

Nair, SK ^{[1
]}

Georg, GI ^{[1
]}

机构：

[1] Univ Kansas, Dept Med Chem, Lawrence, KS 66045 USA

来源：

ORGANIC LETTERS | 2001年 / 3卷 / 12期

关键词：

D O I：

10.1021/ol010044s

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

[GRAPHICS] An efficient, concise approach to the macrolide core of the cryptophycins, potent antimitotic agents, has been achieved, The reaction sequence features a novel macrolactonization utilizing a reactive acyl-beta -lactam intermediate that incorporates the p amino acid moiety within the 16-membered macrolide core. This highly modular approach, which allows for multiple alterations throughout the structure, was successfully applied to the total synthesis of cryptophycin-24.

引用

页码：1813 / 1815

页数：3

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[11] Intramolecular aminolysis of trichloroethyl esters: a mild macrocyclization protocol for the preparation of cryptophycin derivatives [J].