Patent Number: 6,169,177

Title: Processes for the synthesis of oligomeric compounds

Abstract: The present invention provides synthetic processes by which oligomeric compounds, having at least one phosphodiester or phosphorothioate linkage, are prepared. The synthetic processes use a novel mixture of concentrated ammonium hydroxide and a thiol compound during the deblocking step of all or selected internucleoside linkages. Alternatively, the deblocking is carried out in two steps using a mercapto compound in an aqueous amine followed by concentrated ammonium hydroxide. Also provided are synthetic intermediates useful in such processes. Novel oxidation procedures to give phosphodiester oligomers are also included.

Inventors: Manoharan; Muthiah (Carlsbad, CA)

Assignee: Isis Pharmaceuticals, Inc.

International Classification: C07H 21/00 (20060101); C07H 021/00 (); C07H 021/02 (); C07H 021/04 ()

Expiration Date: 01/02/2018