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用于固相合成的六种新型光不稳定连接基。1. 制备方法。

Six new photolabile linkers for solid-phase synthesis. 1. Methods of preparation.

作者信息

Akerblom E B, Nygren A S, Agback K H

机构信息

Medicinal Chemistry, Pharmacia & Upjohn AB, Uppsala, Sweden.

出版信息

Mol Divers. 1997;3(3):137-48. doi: 10.1023/a:1009660431758.

Abstract

In the synthesis of combinatorial chemical libraries on solid phase, there is a need to cleave the compounds from the solid support before the library can be tested for biological activity. It is advantageous to use linkers which will release the libraries by mild photolytic cleavage. We have developed six new linkers of the photosensitive alpha-methyl 2-nitrobenzyl type containing amino, hydroxy, bromo and methylamino groups, and also 4-nitrophenoxycarbonyl activated OH and NH2 groups.

摘要

在固相合成组合化学文库时,在对文库进行生物活性测试之前,需要将化合物从固相载体上裂解下来。使用能通过温和光解裂解来释放文库的连接子是有利的。我们已开发出六种新型的光敏α-甲基-2-硝基苄基型连接子,它们含有氨基、羟基、溴和甲氨基,还有4-硝基苯氧基羰基活化的OH和NH2基团。

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