N3'-->P5' Oligodeoxyribonucleotide Phosphoramidates: A New Method of Synthesis Based on a Phosphoramidite Amine-Exchange Reaction.
A new method for the synthesis of N3'-->P5' phosphoramidate oligodeoxynucleotides is demonstrated. Described herein is the synthesis of the monomers utilized in the phosphoramidite amine-exchange process and the experimental details pertaining to this new mode of chain assembly. The phosphoramidite amine-exchange method generates coupling yields in the 92-95% range per cycle and further enables the synthesis of chimeric phosphoramidate/phosphodiester or phosphoramidate/phosphorothioate oligonucleotides with no instrument modifications.
Nelson
Jeffrey S.
JS
Lynx Therapeutics, 3832 Bay Center Place, Hayward, California 94545.
Fearon
Karen L.
KL
Nguyen
Mark Q.
MQ
McCurdy
Sarah N.
SN
Frediani
Jeff E.
JE
Foy
Michael F.
MF
Hirschbein
Bernard L.
BL