Solid-Phase synthesis of endothelin receptor antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 13, Issue 10, 2003, Pages 1721-1724

  Lange, Udo E W ^a,b   Braje, Wilfried M ^b   Amberg, Willi ^b   Kettschau, Georg ^b,c  

^a BASF SE   (Germany)

^b ABBOTT GMBH AND CO KG   (Germany)

^c BAYER PHARMA AG   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

BORONIC ACID DERIVATIVE; BUTYRIC ACID DERIVATIVE; ENDOTHELIN RECEPTOR ANTAGONIST; ETHER DERIVATIVE; PYRIMIDINE DERIVATIVE;

ARTICLE; AUTOMATION; DRUG ACTIVITY; DRUG POTENCY; DRUG SELECTIVITY; DRUG SYNTHESIS; SOLID;

LATEOLABRAX JAPONICUS;

EID: 0038363860     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(03)00236-1     Document Type: Article

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43. The synthesis was carried out on the Myriad core system (Mettler-Toledo). All washing steps and reagent additions were performed in an automated manner. The palladium catalyst was added manually, but could in principle also be added as a suspension on the Myriad core system or as a solid using a dry pipette. All reaction steps were performed under an inert atmosphere of argon. Unless otherwise specified, all solvents and reagents were obtained from commercial suppliers and used without further purification.
44. B assay) in the presence or absence of the test compound. Nonspecific binding was measured with 0.1 μM ET-1.