Synthesis of silicon traceless linker for solid-phase reaction

被引:2
作者
Mun, HS [1 ]
Jeong, JH [1 ]
机构
[1] Kyung Hee Univ, Coll Pharm, Seoul 130701, South Korea
关键词
combinatorial chemistry; traceless linker; silicon linker; solid-phase reaction; Fischer indole synthesis; benzodiazepine; phenothiazine; swelling; solvation;
D O I
10.1007/BF02980075
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The silicon linker is the foremost traceless linker used in solid-phase reactions. Hydrogen fluoride (HF) or trifluoroacetic aicd (TFA) can remove the silicon linker with the silicon atom being replaced by a hydrogen atom. In this experiment, the linkers 1c and 2d, which are the most useful in solid-phase reactions, were synthesized. Linker 1c is composed of seven linearly linked carbons and linker 2d includes an oxygen atom in the linear carbon chain to increase the solvation capacity. The carboxylic acid component of linker 1c and 2d forms an amide or ester bond with resin. The synthesized linkers 1c and 2d could be utilized in constructing a chemical compound library that includes indole, benzodiazepine and phenothiazine (aromatic ring compounds).
引用
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页码:371 / 375
页数:5
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