Solid-phase synthesis of endothelin receptor antagonists |
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Authors: | Lange Udo E W Braje Wilfried M Amberg Willi Kettschau Georg |
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Institution: | BASF AG, D-67056 Ludwigshafen, Germany. udo.lange@abbott.com |
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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. |
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