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Synthesis of carbon‐14 labelled piritrexim ‐ a potential anticancer agent
Author(s) -
Hill John A.,
Wisowaty James C.,
Darnofall Michael E.
Publication year - 1993
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580331206
Subject(s) - chemistry , guanidine , carbon 14 , hydrochloride , pyrimidine , condensation , stereochemistry , chemical synthesis , mechanism of action , combinatorial chemistry , organic chemistry , in vitro , biochemistry , physics , quantum mechanics , thermodynamics
Piritrexim 1 (2,4‐diamino‐6‐(2,5‐dimethoxybenzyl)‐5‐methylpyrido[2,3‐ d ]‐pyrimidine) was synthesized in the [ 14 C]‐labelled form with specific activity 50.8 mCi/mmol suitable for drug metabolism, transport, dispostion and mechanism of action studies. The synthetic sequence involved synthesis of the novel 2‐bromo‐5‐(2,5‐dimethoxybenzyl)‐4‐methyl‐3‐pyridinecarbonitrile and condensation of this compound with [ 14 C]‐guanidine hydrochloride. The radiochemical purity was >98%.