Title of article
Solid-Phase synthesis of endothelin receptor antagonists
Author/Authors
Udo E. W. Lange، نويسنده , , Wilfried M. Braje، نويسنده , , Willi Amberg، نويسنده , , Georg Kettschau، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2003
Pages
4
From page
1721
To page
1724
Abstract
A new solid-phase synthesis for ET receptor antagonists suitable for automation is presented. A support bound 2-hydroxybutyric acid derivative was converted to the corresponding ether derivatives using 4-halo-2-methylsulfonylpyrimidines. Subsequent Suzuki coupling with various aryl boronic acids gave the desired antagonists in good yields and purities. Highly potent antagonists with excellent selectivity for ETA were obtained.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2003
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
793220
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