Synthesis and antifolate properties of 10-alkyl-8, 10-dideazaminopterins

…, RL Kisliuk, Y Gaumont, FM Sirotnak

Index: DeGraw; Christie; Brown; Kelly; Kisliuk; Gaumont; Sirotnak Journal of Medicinal Chemistry, 1984 , vol. 27, # 3 p. 376 - 380

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Citation Number: 17

Abstract

of sodium cyanide was found to cause ester cleavage and decarboxylation after heating for 1-2 h. The starting diester, 2a, could be alkylated with lower alkyl halides to afford the dimethyl a-alkylhomoterephthalates 2b-d. These were alkylated with the bromide 1 in the manner described above and similarly decarboxylated to give the desired 4-amino-4-deoxy- 10-alky1-8, 10-dideazapteroic acid analogues 4b-d. Coupling with diethyl L-glutamate, ...