| Autor: | Catherine C.K. Yuan, Stephen T. Ross, Fadia E. Ali, Leon B. Hall |
|---|---|
| Rok vydání: | 2000 |
| Předmět: |
Primary (chemistry)
Combinatorial Chemistry Techniques Chemistry Organic Chemistry Regioselectivity General Medicine Nuclear magnetic resonance spectroscopy Alkylation Combinatorial chemistry Catalysis Inorganic Chemistry Position (vector) Heck reaction Drug Discovery Organic chemistry Molecule Physical and Theoretical Chemistry Molecular Biology Information Systems |
| Zdroj: | Molecular Diversity. 5:1-5 |
| ISSN: | 1381-1991 |
| Popis: | An efficient solid phase regioselective alkylation at the N4 position of a 3-oxo-1,4-benzodiazepine template exemplified by 4-H-2,3,4,5-tetrahydro-7-iodo-3-oxo-1H-1,4-benzodiazepine-2-acetate-polymer ester is described. Further chemical elaboration at position 7, utilizing a modified Heck reaction, allows the incorporation of amides from primary or secondary amines. The two diversity points at positions 4 and 7 were utilized to synthesize a 28-membered, combinatorial array on Sasrin resin in moderate yields and > 80% purity. Having validated the chemistry on solid support, a combine and split approach to prepare a bead-bound combinatorial library is achievable utilizing similar experimental practices and procedures as in the array synthesis. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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