Abstract
An expeditious synthesis of LY288601 (2), the 5,6-dihydro analog of the pyrrolo[2,3-d]pyrimidine-based antifolate compound LY231514 (1a), is described. The synthesis proceeds in eight steps from tert-butyl 4-iodobenzoate and involves the elaboration of a 2-amino-4-hydroxypyrmidine ring onto an activated 3-carboalkoxy-2-pyrrolidinone via reaction with guanidine as a key step
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