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An improved three-step synthesis of N2-alkylated guanines has been developed starting from N2-Boc-protected 2-amino-6-chloropurine which was treated with Boc2O, and the resulting doubly N2,9-protected derivative was subjected to N2-alkylation with alkyl halides, followed by hydrolysis. The advantages of this procedure include short reaction steps, simple operations, and good yields.
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