Synthesis of the 7-hydroxy metabolites of methotrexate and 10-ethyl-10-deazaaminopterin
The potent folate antagonists methotrexate and 10-ethyl-10-deazaaminopterin are oxidized in vivo to their 7-hydroxy derivatives. A specific cyanation at the C-7 position of the pteridine ring system using diethyl phosphorocyanidate converted the dimethyl esters of methotrexate and 10-ethyl-10-deazaaminopterin to the corresponding 7-cyano dimethyl ester derivatives, which were hydrolyzed to the 7-hydroxy metabolites.
Dawson,O'Krongly,Hobbs,Barrueco,Sirotnak
p. 635 - 638
(2007/10/02)
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