The synthesis and biological activity of a series of 2,4-diaminopyrido[2,3- D]pyrimidine based antifolates as antineoplastic and antiarthritic agents

Abstract

A new series of 2,4-diaminopyrido[2,3- d]pyrimidine based antifolates 1–3 were synthesized through an efficient conversion of 2-pivaloyl-4-oxo-6-ethynylpyrido[2,3- d]pyrimidine 5 to the corresponding 4-amino analog 7 via the activated 1,2,4-triazole intermediate 6. Compound 7 was used as the key intermediate for the preparation of the final products. The detailed biological evaluation of these compounds both as antineoplastic and antiarthritic agents will be discussed.