Antitumour imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl) imidazo [5, 1-d]-1, 2, 3, 5-tetrazin-4 (3H)-one, a novel broad-spectrum …

MFG Stevens, JA Hickman, R Stone…

Index: Stevens, Malcolm F. G.; Hickman, John A.; Stone, Robert; Gibson, Neil W.; Baig, Ghouse Unissa; et al. Journal of Medicinal Chemistry, 1984 , vol. 27, # 2 p. 196 - 201

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Citation Number: 200

Abstract

Interaction of 5-diazoimidazole-4-carboxamide and alkyl and aryl isocyanates in the dark affords 8-carbamoyl-3-substituBd-imidazo [5, 1-d]-1, 2, 3, 5-tetraz~-4 (3~-ones. In cold methanol or ethanol, the 3-(2-chloroethyl) derivative 7a decomposes to afford 2- azahypoxanthine (14) and methyl and ethyl N-(2-chloroethyl) carbamates, respectively. Compound 7a has curative activity against L-1210 and P388 leukemia and may act as a ...