Synthesis and biological evaluation of 5-deazaisofolic acid, 5-deaza-5,6,7,8-tetrahydroisofolic acid, and their N9-substituted analogues.

@article{Singh1991SynthesisAB,
  title={Synthesis and biological evaluation of 5-deazaisofolic acid, 5-deaza-5,6,7,8-tetrahydroisofolic acid, and their N9-substituted analogues.},
  author={S. Singh and I. Dev and D. Duch and R. Ferone and G. K. Smith and J. Freisheim and J. Hynes},
  journal={Journal of medicinal chemistry},
  year={1991},
  volume={34 2},
  pages={
          606-10
        }
}
  • S. Singh, I. Dev, +4 authors J. Hynes
  • Published 1991
  • Chemistry, Medicine
  • Journal of medicinal chemistry
  • Prompted by recent disclosures concerning the potent antitumor activities of 5-deaza-5,6,7,8-tetrahydrofolic acid and 5,10-dideaza-5,6,7,8-tetrahydrofolic acid (DDATHF), we have prepared 5-deazaisofolic acid (3a) and 5-deaza-5,6,7,8-tetrahydroisofolic acid (4a). Reductive condensation of 2,6-diamino-3,4-dihydro-4- oxopyrido[2,3-d]pyrimidine with di-tert-butyl N-(4-formylbenzoyl)-L-glutamate and subsequent deprotection with trifluoroacetic acid yielded 5-deazaisofolic acid in good yield… CONTINUE READING
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