The solid-phase synthesis and use of N-monosubstituted piperazines in chemical library synthesis.
J Comb Chem
; 5(3): 260-6, 2003.
Article
em En
| MEDLINE
| ID: mdl-12739942
ABSTRACT
An efficient solid-phase synthesis of mono-N-substituted piperazines is presented. The key transformation involves a selective borane amide bond reduction in the presence of a carbamate resin linkage. This synthetic route takes advantage of the large diverse pool of commercially available carboxylic acids, acid chlorides, and sulfonyl chlorides. The solid-phase approach facilitates parallel processing by eliminating the need for column chromatography after each synthetic step. The N-monosubstituted piperazines were shown to react with polymeric activated tetrafluorophenol (TFP) reagents to generate arrays of amides and sulfonamides in good purity for biological testing.
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Base de dados:
MEDLINE
Idioma:
En
Ano de publicação:
2003
Tipo de documento:
Article
País de afiliação:
Estados Unidos