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The aptameric protective group strategy for the one-step regioselective transformation of aminoglycoside antibiotics was found to be compatible with diverse reagents and reaction conditions. New derivatives of neomycin B were synthesized with regioselectivities of >99%. This result extends the scope of applicability of APGs facilitating access to novel aminoglycoside derivatives.

Graphical abstract: Aptamer protective groups tolerate different reagents and reactions for regioselective modification of neomycin B

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