Details

Autor(en) / Beteiligte

• Cheng, Ming-Fu
• Fang, Jim-Min

Titel

Liquid-Phase Combinatorial Synthesis of 1,4-Benzodiazepine-2,5-diones as the Candidates of Endothelin Receptor Antagonism

Ist Teil von

• Journal of combinatorial chemistry, 2004-01, Vol.6 (1), p.99-104

Ort / Verlag

United States: American Chemical Society

Erscheinungsjahr

2004

Quelle

MEDLINE

Beschreibungen/Notizen

• A library of 1,4-benzodiazepine-2,5-dione dicarboxylate derivatives containing aryl substituents at N 1- and N 4-positions to mimic the amino acid residues of Try-13, Phe-14, and Asp-18 in endothelin-1 is established by using the starting materials of α-amino esters, hydroxybenzaldehydes, nitrobenzoyl chlorides, and benzyl bromides in a polyethylene resin-bound liquid-phase synthesis. All of the six synthetic steps are conducted under mild conditions to give the desired products with reasonable yields and purity. The poly(ethylene glycol) support plays as a part of ester linkage that is released at the final step.