用于固相合成的非酸性可降解连接基。

A nonacid degradable linker for solid-phase synthesis.

作者信息

Colombo Aina, De la Figuera Natalia, Fernàndez Joan Carles, Fernández-Forner Dolors, Albericio Fernando, Forns Pilar

机构信息

Almirall-Barcelona Science Park Unit, Josep Samitier 1-5, E-08028 Barcelona, Spain.

出版信息

Org Lett. 2007 Oct 11;9(21):4319-22. doi: 10.1021/ol701879s. Epub 2007 Sep 15.

DOI:10.1021/ol701879s

PMID:17867699

Abstract

Synthesis and applications of two new nonacid degradable linkers as an alternative to the Wang linker for solid-phase synthesis are described. Resin from linker 2 looks superior to linker 1 in terms of yields for both anchoring of the first building block and cleavage and in terms of higher purity of the final product. Use of linker 2 avoids side reactions associated with the use of Wang resin due to an undesired cleavage during final acid treatment.

摘要

描述了两种新型非酸可降解连接体的合成及其作为用于固相合成的Wang连接体替代品的应用。就第一个结构单元的锚定和裂解产率以及最终产物的更高纯度而言，连接体2的树脂看起来优于连接体1。使用连接体2可避免因最终酸处理期间的意外裂解而与使用Wang树脂相关的副反应。