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Highly Efficient Synthesis of DNA-Binding Polyamides Using a Convergent Fragment-Based Approach

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journal contribution
posted on 05.09.2014, 00:00 by Andrew J. Fallows, Ishwar Singh, Ruggero Dondi, Paul M. Cullis, Glenn A. Burley
Two advances in the synthesis of hairpin pyrrole-imidazole polyamides (PAs) are described. First, the application of a convergent synthetic strategy is shown, involving the Boc-based solid phase synthesis of a C-terminal fragment and the solution phase synthesis of the N-terminal fragment. Second a new hybrid resin is developed that allows for the preparation of hairpin PAs lacking a C-terminal β-alanine tail. Both methods are compatible with a range of coupling reagents and provide a facile, modular route to prepare PA libraries in high yield and crude purity.

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