2,4-Diamino-5-benzylpyrimidines and analogues as antibacterial agents. 2. C-Alkylation of pyrimidines with Mannich bases and application to the synthesis of trimethoprim and analogues
| Autor: | Barbara Roth, Justina Z. Strelitz, Barbara S. Rauckman |
|---|---|
| Rok vydání: | 1980 |
| Předmět: |
Pyrimidine
Alkylation Bacteria Chemistry Stereochemistry Atom (order theory) Microbial Sensitivity Tests In Vitro Techniques Combinatorial chemistry Trimethoprim Anti-Bacterial Agents Rats Mannich Bases chemistry.chemical_compound Structure-Activity Relationship Drug Discovery medicine Escherichia coli Molecular Medicine Animals Folic Acid Antagonists Antibacterial agent medicine.drug |
| Zdroj: | Journal of medicinal chemistry. 23(4) |
| ISSN: | 0022-2623 |
| Popis: | A new route to 5-(p-hydroxybenzyl)pyrimidines has been developed which utilizes phenolic Mannich bases plus pyrimidines containing at least two activating groups. The products can be alkylated on the phenolic oxygen or on the pyrimidine N-1 atom, depending on conditions. This method has been used to prepare trimethoprim, a broad-spectrum antibacterial agent, starting from 2,4-diaminopyrimidine and 2,6-dimethoxyphenol. |
| Databáze: | OpenAIRE |
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