2,4-Diamino-5-benzylpyrimidines and analogs as antibacterial agents. 2. C-Alkylation of pyrimidines with Mannich bases and application to the synthesis of trimethoprim and analogs

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...

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Veröffentlicht in:	Journal of medicinal chemistry 1980-04, Vol.23 (4), p.379-384
Hauptverfasser:	Roth, Barbara, Strelitz, Justina Z, Rauckman, Barbara S
Format:	Artikel
Sprache:	eng
Schlagworte:	Alkylation Animals Anti-Bacterial Agents - chemical synthesis Bacteria - drug effects Escherichia coli - drug effects Escherichia coli - enzymology Folic Acid Antagonists In Vitro Techniques Mannich Bases Microbial Sensitivity Tests Rats Structure-Activity Relationship Trimethoprim - analogs & derivatives Trimethoprim - chemical synthesis Trimethoprim - pharmacology
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