Linkers for solid-phase synthesis of small molecules: coupling and cleavage techniques

被引：11

作者：

Eggenweiler, HM ^{[1
]}

机构：

[1] Merck KGaA, Med Chem, Res Labs, D-64271 Darmstadt, Germany

来源：

DRUG DISCOVERY TODAY | 1998年 / 3卷 / 12期

关键词：

D O I：

10.1016/S1359-6446(98)01265-3

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Combinatorial chemistry has an impact on lead discovery as well as on lead optimization. The efficient synthesis of individual compounds, which has replaced the initial goal of synthesizing highly complex mixtures, can be carried out in solution or on a suitable support material. The role of a linker in solid-phase chemistry is to connect the starting material reversibly with the solid support. The main challenges in choosing an appropriate linker molecule are that the starting compounds can be easily attached to it, that it is chemically stable in the envisaged synthesis conditions and that it should be possible to cleave the final products with high efficiency.

引用

页码：552 / 560

页数：9

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