Abstract
Synthesis of a new tetrahydrobenzodiazepinone analogs as anti-HIV agent was accomplished. First, 8-bromo-9-(2-chloroethoxymethyl)adenine (10) was prepared by treatment of 6-amino-9-(2-chloroethoxymethyl)purine (7) with bromine in NaOAc buffer solution (0.30 M) and 1,4-dioxane. Nucleophilic substitution of the chlorine atom in 10 produced iodo derivative 12. Reaction of 10 with methoxy or hydroxy group gave derivatives 13 and 15, respectively. Cyclization of compound 13 was performed by addition of catalytic amout of (NH4)2SO4 in hexamethyldisilazane.