Lynx Therapeutics, Inc.

Jeffery S Nelson

Sergei M Gryaznov

Karen L Fearon

Ronald G Schultz

Bernard L Hirschbein

Sarah N McCurdy

The invention provides a method of synthesizing oligonucleotide N3'.fwdarw.P5' phosphoramidates using an amine-exchange reaction of phosphoramidites in which a deprotected 3'-amino group of a solid phase supported oligonucleotide chain is exhanged for the amino portion of a 5'-phosphoramidite of an incoming monomer which has a protected 3'-amino group. The resulting internucleotide phosphoramidite linkage is then oxidized to form a stable protected phosphoramidate linkage. The method of the invention greatly improves product yields and reduces reagent usage over currently available methods for synthesizing the above class of compound.

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Fremont, CA, United States of America

Jeffery S Nelson