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Bioorg Med Chem Lett. 2003 May 19;13(10):1721-4.

Solid-phase synthesis of endothelin receptor antagonists.

Author information

1
BASF AG, D-67056 Ludwigshafen, Germany. udo.lange@abbott.com

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.

PMID:
12729650
DOI:
10.1016/s0960-894x(03)00236-1
[Indexed for MEDLINE]

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