FURTHER EVALUATION OF 5-ALKYL-5-DEAZA ANTIFOLATES. 5-PROPYL- AND 5-BUTYL-5-DEAZA ANALOGUES OF AMINOPTERIN AND METHOTREXATE

@article{Piper1995FURTHEREO,
  title={FURTHER EVALUATION OF 5-ALKYL-5-DEAZA ANTIFOLATES. 5-PROPYL- AND 5-BUTYL-5-DEAZA ANALOGUES OF AMINOPTERIN AND METHOTREXATE},
  author={J. R. Piper and B. Ramamurthy and C. A. Johnson and J. Maddry and G. Otter and F. M. Sirotnak},
  journal={Journal of Heterocyclic Chemistry},
  year={1995},
  volume={32},
  pages={1205-1212}
}
5-Propyl-5-deaza and 5-butyl-5-deaza analogues of classical antifolates were synthesized by extensions of a previously reported general route which proceeds through 2,4-diamino-5-alkylpyrido[2,3-d]pyrimidine-6-carbonitrile intermediates followed by reductive condensation with diethyl N-4-(aminobenzoyl)-L-glutarnate to give diethyl esters of 5-alkyl-5-deazaaminopterin types. N10-Methyl derivatives, i.e., derivatives of 5-alkyl-5-deazamethotrexate, were also prepared by reductive methylation of… Expand
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