title: N3'-->P5' Oligodeoxyribonucleotide Phosphoramidates: A New Method of Synthesis Based on a Phosphoramidite Amine-Exchange Reaction.
abstract: 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.
authors.affiliation: Lynx Therapeutics, 3832 Bay Center Place, Hayward, California 94545.
authors.forename: Jeffrey S.
authors.initials: JS
authors.lastname: Nelson
authors.forename: Karen L.
authors.initials: KL
authors.lastname: Fearon
authors.forename: Mark Q.
authors.initials: MQ
authors.lastname: Nguyen
authors.forename: Sarah N.
authors.initials: SN
authors.lastname: McCurdy
authors.forename: Jeff E.
authors.initials: JE
authors.lastname: Frediani
authors.forename: Michael F.
authors.initials: MF
authors.lastname: Foy
authors.forename: Bernard L.
authors.initials: BL
authors.lastname: Hirschbein