Liquid-Phase Combinatorial Synthesis of 1,4-Benzodiazepine-2,5-diones as the Candidates of Endothelin Receptor Antagonism
| Autor: | Ming-Fu Cheng, Jim-Min Fang |
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| Rok vydání: | 2003 |
| Předmět: |
Endothelin Receptor Antagonists
Magnetic Resonance Spectroscopy medicine.drug_class Liquid phase Polyethylene Glycols chemistry.chemical_compound medicine Combinatorial Chemistry Techniques Organic chemistry Chromatography High Pressure Liquid Benzodiazepinones Benzodiazepine Hydrolysis Aryl General Chemistry Polyethylene Combinatorial synthesis chemistry Solvents Indicators and Reagents Spectrophotometry Ultraviolet Chromatography Thin Layer Polyethylenes Antagonism Endothelin receptor Ethylene glycol |
| Zdroj: | Journal of Combinatorial Chemistry. 6:99-104 |
| ISSN: | 1520-4774 1520-4766 |
| DOI: | 10.1021/cc030034d |
| Popis: | 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 alpha-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. |
| Databáze: | OpenAIRE |
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