Abstract
AbstractSeveral 5‐(4‐substituted benzyl)‐2,4‐diaminoquinazolines were prepared as potentially selective inhibitors of Candida albicans dihydrofolate reductase. These compounds were synthesized by a novel route, which included as a key step the displacement of a fluoro group in 2,6‐difluorobenzonitrile by the anions of ethyl or methyl 4‐substituted phenylacetates. The resultant diarylacetates were saponified and decarboxylated to the 2‐fluoro‐6‐(4‐substituted phenyl)benzonitriles. Ring closure of these benzonitriles with guanidine carbonate gave the 5‐(4‐substituted benzyl)‐2,4‐diaminoquinazolines.
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