Abstract
AbstractThe ability of 2‐amino‐4‐hydroxy‐7H‐pyrimido[4,5‐b][1,4]oxazine derivatives to inhibit dihydrofolate reductase led to a search for means of synthesizing new side chain substituted analogs of this marginally stable pyrimidooxazine system. A study of the synthesis and use of 6‐functionalized pyrimido[4,5‐b][1,4]oxazines for coupling side chains was begun and has now revealed methods for coupling p‐aminobenzoic acid with 2‐amino‐4‐hydroxy‐6‐carboxy‐7H‐pyrimido[4,5‐b][1,4]oxazine and hydrolyzed 2‐amino‐4‐hydroxy‐6‐carbe‐thoxymethylene‐6,7‐dihdyro‐5H‐pyrimido[4,5‐b][1,4]oxazine. The products are of interest for evaluation as potential antifolates.
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