Solid-phase synthesis of aryl-alkylamine derivatives using protected aminoalcohol building blocks on SynPhaseTM lanterns

被引：5

作者：

Zajdel, Pawel

Subra, Gilles

Pawlowski, Maciej

Martinez, Jean

机构：

[1] Univ Montpellier I, Fac Pharm, LAPP, UMR 5810, F-34060 Montpellier, France

[2] Univ Montpellier 2, Fac Pharm, LAPP, UMR 5810, F-34060 Montpellier, France

[3] Jagiellonian Univ, Coll Med, Dept Med Chem, PL-30688 Krakow, Poland

来源：

QSAR & COMBINATORIAL SCIENCE | 2007年 / 26卷 / 02期

关键词：

aminoalcohols; arylpiperazines; BAL linker; 5-HT1A; 5-HT7; D-3; D-4 receptor ligands; solid-phase synthesis;

D O I：

10.1002/qsar.200620036

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of aryl-alkylamine carboxamide and sulfonamide derivatives were synthesized on a BAL linker using SynPhase (TM) Lanterns. All the reaction steps were performed on a solid support. The key stage was on-resin substitution of TBDPSi-protected aminoalcohols with various amines, which circumvented the multistep solution-phase synthesis of alkylamine building blocks. The chemistry applied allows building up focused libraries targeted on CNS receptors.

引用

页码：215 / 219

页数：5

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