Synthesis and antifolate properties of 9-alkyl-10-deazaminopterins

…, PH Christie, RL Kisliuk, Y Gaumont…

Index: DeGraw; Christie; Kisliuk; Gaumont; Sirotnak Journal of Medicinal Chemistry, 1990 , vol. 33, # 1 p. 212 - 215

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Citation Number: 11

Abstract

Reformatski condensation of benzyl 2-bromopropionate with 4-~ arbomethoxybenzaldehyde , followed by dehydration afforded benzyl 2-methyl-p-carbomethoxycinnamate (4a). Hydrogenation over a Pd catalyst gave the hydrocinnamic acid 5a. Conversion to the chloromethyl (6a) and azidomethyl ketone (7a) was followed by hydrogenation to the aminomethyl ketone@ a). Direct N-alkylation by 2, 4-diamino-5-nitro-6-chloroppimidine ...