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Synthesis of carbon-14 labelled piritrexim - a potential anticancer agent

✍ Scribed by John A. Hill; James C. Wisowaty; Michael E. Darnofall

Publisher
John Wiley and Sons
Year
1993
Tongue
French
Weight
493 KB
Volume
33
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

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%.

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