Synthesis and antifolate properties of 10-alkyl-8,10-dideazaminopterins

Article abstract of DOI:10.1021/jm00369a024

The synthesis of 10-alkyl analogues of the potent antitumor agent 8,10-dideazaminopterin is described. Alkylation of appropriate α-alkyl homoterephthalate esters with 2,4-diamino-6-(bromomethyl)-8-deazapteridine afforded 10-alkyl-10-carboxy-4-amino-4-deox