Synthesis and antifolate evaluation of 10-ethyl-5-methyl-5, 10-dideazaaminopterin and an alternative synthesis of 10-ethyl-10-deazaaminopterin (edatrexate)

…, CA Johnson, GM Otter, FM Sirotnak

文献索引：Piper; Johnson; Otter; Sirotnak Journal of Medicinal Chemistry, 1992 , vol. 35, # 16 p. 3002 - 3006

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被引用次数: 23

摘要

3004 Journal of Medicinal Chemistry, 1992, Vol. 35, No. 16 5-methyl (2), 17 10-methyl (3), 18J9 10-ethyl (4), 18 and 5, lO-ethylene-bridged (S) 20 compounds are known, but no 5, lO- dialkyl representative from this series has been reported. We regarded the 5, lO-dialkyl type derivative as an important prospective series which warranted study. The representative selected for synthesis was the 5-methyl-10-ethyl derivative 12a (Scheme I). Chemistry. ...