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Synthesis and antiviral activity of 9-[4-hydroxy-3-(hydroxymethyl) but-1-yl] purines

MR Harnden, RL Jarvest, TH Bacon…

文献索引:Harnden, Michael R.; Jarvest, Richard L.; Bacon, Teresa H.; Boyd, Malcolm R. Journal of Medicinal Chemistry, 1987 , vol. 30, # 9 p. 1636 - 1642

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被引用次数: 176

摘要

Alkylation of 2-amino-6-chloropurine with 5-(2-bromoethyl)-2, 2-dimethyl-1, 3-dioxane (5) provided 2-amino-6-chloro-9-[2-(2, 2-dimethyl-l, 3-dioxan-5-yl) ethyl] purine (6) in high yield. This aminochloropurine 6 was readily converted to the antiviral acyclonucleoside 9-[4- hydroxy-3-(hydroxymethyl) but-l-yl] guanine (1) and to its 6-chloro (IO), 6-thio (Il), 6-alkoxy (12-17), 6-amino (20), and 6-deoxy (21) purine analogues. The guanine derivative 1 was ...