Efficient functionalization of 2-amino-6-chloropurine derivatives at C-8 via 8-lithiated species
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Add time:09/24/2019 Source:sciencedirect.com
9-Substituted 2-amino-6-chloropurines are important intermediates in the synthesis of a variety of purine and purine nucleoside derivatives, and were efficiently halogenated, alkylated and formylated at the C-8 position via lithiation of N2 mono THP protected purines. Notably, even fluoride could be introduced to the purine 8-position, but in a modest yield. Lithiation of non-protected 2-amino-6-chloropurines led to a ring-opening of the pyrimidine ring.
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