Isis Pharmaceuticals, Inc.

Nitto-denko Corporation

Isis Pharmeuticals, Inc.

Vasulinga T Ravikumar

Douglas L Cole

Daniel C Capaldi

Zacharia S Cheruvallath

Muthiah Manoharan

Andrei P Guzaev

Achim H Krotz

Raju K Kumar

Zhiwei Wang

Dennis Mulvey

Richard Holmes Griffey

Phillip Dan Cook

Venkatraman Mohan

Tatsuya Konishi

Gang Zhao

Mark Andrade

Ayako Matsunawa

Takeo Matsumura

Muthia Manoharan

Kenjirou Mori

Cheiko Kitaura

Thazha P Prakash

Balkrishen Bhat

Alessandra Eleuteri

Achim Krotz

Universal linkers, their facile processes of manufacture and methods of using the same are provided.

Supports for oligomer synthesis

The present invention provides an improved process for the synthesis of 2'-O-substituted purine nucleosides. The process includes anhydro or thioanhydro ring opening of a selected 8,2&#x2032;-cyclopurine nucleoside with a weak nucleophile in the presence of a Lewis acid ester, followed by reduction to afford the desired 2&#x2032;-O-substituted purine nucleoside.

Process for the synthesis of 2'-O-substituted purine nulceosides

Methods for the formation of sulfurized oligonucleotides are provided. The methods allow for the formation of phosphorothioate linkages in the oligonucleotides or derivatives, without the need for complex solvent mixtures and repeated washing or solvent changes. Oligonucleotides having from about 8, and up to about 50, nucleotides can be sulfurized according to the methods of the invention with higher yields than have been previously reported.

Synthesis of sulfurized oligonucleotides

The present invention provides solid support media for use in oligomer synthesis, methods of producing the media, and methods of using the media. In some embodiments, the processes of the invention comprise (a) providing an organic phase comprising an olefin monomer, a cross-linker, a functionalizing reagent and an initiator; and (b) contacting the organic phase with an aqueous phase under conditions of time and temperature effective to form the polymeric bead.

Polymeric beads for oligomer synthesis

Improved methods for synthesis of oligonucleotides and other phosphorus-linked oligomers are disclosed. The methods include the use of aromatic solvents, alkyl aromatic solvents, halogenated aromatic solvents, halogenated alkyl aromatic solvents, or aromatic ether solvents to achieve deprotection of protected hydroxyl groups.

Methods for synthesis of oligonucleotides

Synthetic processes are provided wherein oligomeric compounds are prepared having phosphodiester, phosphorothioate, phosphorodithioate, or other covalent linkages. The oligomers have substantially reduced exocyclic adducts deriving from acrylonitrile or related contaminants.

Process for the synthesis of oligomeric compounds

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Carlsbad, CA, United States of America

Vasulinga T Ravikumar