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Solid Phase Synthesis of a Functionalized Bis-Peptide Using "Safety Catch" Methodology
Published on: May 15, 2012
Solid-phase synthesis of endothelin receptor antagonists
Udo E W Lange1, Wilfried M Braje, Willi Amberg
1BASF AG, D-67056 Ludwigshafen, Germany. udo.lange@abbott.com
Bioorganic & Medicinal Chemistry Letters
|May 6, 2003
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 ET(A) were obtained.

