Abstract (6R, 6S)-5, 8-Dideaza-5, 6, 7, 8-tetrahydroaminopterin (1) and (6R, 6S)-5, 8- dideaza-5, 6, 7, 8-tetrahydromethotrexate (2) were synthesized as potential inhibitors of dihydrofolate reductase (DHFR) and as antitumor agents. Cyclohexanone-4- carboxaldehyde dimethyl acetal, a key intermediate [10] was synthesized from cyclohexane- 1, 4-dione monoethylene ketal, which was converted via a Wittig reaction to its exocyclic 4 ...