Synthesis and Antifolate Properties of 10-Alkyl-5,10-dideaza Analogues of Methotrexate and Tetrahydrofolic Acid

Article abstract of DOI:10.1021/jm00164a033

Synthesis of the 10-methyl and 10-ethyl analogues of 5,10-dideazatetrahydrofolic acid (DDTHF), a potent inhibitor of glycinamide ribotide (GAR) formyltransferase, is reported.Key intermediates in the process were 10-methyl- and 10-ethyl-4-amino-4-deoxy-5,