An improved synthesis of oligodeoxynucleotide N3′→ P5′ phosphoramidates and their chimera using hindered phosphoramidite monomers and a novel handle for …

KL Fearon, BL Hirschbein, JS Nelson…

Index: Nelson, Jeffrey S.; Fearon, Karen L.; Nguyen, Mark Q.; McCurdy, Sarah N.; Frediani, Jeff E.; Foy, Michael F.; Hirschbein, Bernard L. Journal of Organic Chemistry, 1997 , vol. 62, # 21 p. 7278 - 7287

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Citation Number: 19

Abstract

Abstract Oligodeoxynucleotide N3′→ P5′ phosphoramidates are promising candidates for antisense therapeutics, as well as for diagnostic applications. We recently reported a new method for the synthesis of these oligonucleotide analogs which makes use of a phosphoramidite amine-exchange reaction in the key coupling step. We report herein an improved set of monomers that utilize a more reactive, hindered phosphoramidite to ...

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