Regioselective N9 alkylation of purine rings assisted by β-cyclodextrin
Under the assistance of β-cyclodextrin, purine was effectively alkylated at N9 together with up to 99% conversion and good to excellent yield using water as the solvent. High regioselectivity-N9/N7 selectivity>99:1 was attributed to the β-cyclodextrin cav
Antitumor Agents. 86. Synthesis and Cytotoxicity of α-Methylene-γ-lactone-Bearing Purines
α-Methylene-γ-lactones covalently linked to adenine (3), hypoxantine (4), and guanine (5) were synthesized by using the convenient Reformatsky-type reaction between ethyl α-(bromomethyl)acrylate and the proper purine ketones.In vitro cytotoxicity data demonstrated that these compounds were active against L-1210 tissue culture cells with 3 being most potent (ED50 = 0.3 μg/mL).