Synthesis and evaluation of a classical 2, 4-diamino-5-substituted-furo [2, 3-d] pyrimidine and a 2-amino-4-oxo-6-substituted-pyrrolo [2, 3-d] pyrimidine as antifolates

A Gangjee, J Yang, JJ McGuire, RL Kisliuk

文献索引：Gangjee, Aleem; Yang, Jie; McGuire, John J.; Kisliuk, Roy L. Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 24 p. 8590 - 8598

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被引用次数: 29

摘要

Two classical antifolates, a 2, 4-diamino-5-substituted furo [2, 3-d] pyrimidine and a 2-amino- 4-oxo-6-substituted pyrrolo [2, 3-d] pyrimidine, were synthesized as potential inhibitors of dihydrofolate reductase (DHFR) and thymidylate synthase (TS). The syntheses were accomplished by condensation of 2, 6-diamino-3 (H)-4-oxo-pyrimidine with α-chloro-ketone 21 to afford two key intermediates 23 and 24, followed by hydrolysis, coupling with l- ...