Chemical synthesis and biological activities of 5-deazaaminopterin analogs bearing substituent (s) at the 5-and/or 7-position (s)

…, GM Otter, FM Sirotnak, KA Watanabe

Index: Su; Huang; Chou; Otter; Sirotnak; Watanabe Journal of Medicinal Chemistry, 1988 , vol. 31, # 6 p. 1209 - 1215

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Citation Number: 17

Abstract

Condensation of cyanothioacetamide (4) with ethyl a-(ethoxymethy1ene) acetoacetate (5b), ethyl 4-ethoxy-2-(eth-oxymethylene)-3-oxobutanoate (5c), ethyl 2-(ethoxymethylene)-3-oxo- 4-phenylpropanoate (5d) afforded exclusively the corresponding 6-substituted pyridines (6b- d). Cyclization of 4 with 3-carbethoxybutane-2, 4-dione (5e) gave 3-cyano-5- (ethoxycarbonyl)-4, 6-dimethylpyridine-2 (l~-thione (6e), whereas reaction of 4 with 3- ...