Synthesis and Antifolate Activity of 5-Methyl-5,10-dideaza Analogues of Aminopterin and Folic Acid and an Alternative Synthesis of 5,10-Dideazatetrahydrofolic Acid, a Potent Inhibitor of Glycinamide Ribonucleotide Formyltransferase

Article abstract of DOI:10.1021/jm00119a018

The title compounds were prepared in extensions of a general synthetic approach used earlier to prepare 5-alkyl-5-deaza analogues of classical antifolates.Wittig condensation of 2,4-diaminopyrido<2,3-d>pyrimidine-6-carboxaldehyde (2a) and its 5-methyl ana