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.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Lange UE,Braje WM,Amberg W,Kettschau Gdoi
10.1016/s0960-894x(03)00236-1subject
Has Abstractpub_date
2003-05-19 00:00:00pages
1721-4issue
10eissn
0960-894Xissn
1464-3405pii
S0960894X03002361journal_volume
13pub_type
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