Synthesis of a 2, 4, 8-Trisubstituted Pyrimidino[5, 4-d]Pyrimidine Library via Sequential SNAr Reactions on Solid-Phase
| Autor: | Moustafa E. El-Araby, M. R. Player, Richard S. Pottorf |
|---|---|
| Rok vydání: | 2004 |
| Předmět: |
Magnetic Resonance Spectroscopy
Pyrimidine Organic Chemistry General Medicine Combinatorial chemistry Computer Science Applications Structure-Activity Relationship chemistry.chemical_compound Pyrimidines chemistry Nucleophilic aromatic substitution Phase (matter) Yield (chemistry) Drug Discovery Combinatorial Chemistry Techniques Organic chemistry Indicators and Reagents |
| Zdroj: | ResearcherID |
| ISSN: | 1386-2073 |
| DOI: | 10.2174/1386207043328571 |
| Popis: | A solid-phase synthesis of 2, 4, 8-substituted pyrimidino[5, 4-d]pyrimidines involving three controlled S(N)Ar reactions has been developed. Exploration of different heterocyclic starting materials and resin-bound intermediates is highlighted. The preferred method starts with the treatment of resin-bound anilines with 2, 4, 8-trichloropyrimidino[5, 4-d]pyrimidine. This intermediate is subsequently treated with various amines in two steps to yield the final products. The scope of each diversity step was determined and a library of 16, 000 compounds was synthesized. |
| Databáze: | OpenAIRE |
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