Method of synthesizing sulfurized oligonucleotide analogs
AssigneeLynx Therapeutics, Inc.
InventorsWojciech J. Stec, Bogdan Uznanski, B. John Bergot, Bernard L. Hirschbein, Karen L. Fearson
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Abstract
A method for synthesizing sulfurized oligonucleotide analogs, such as phosphorothioate and phosphorodithioate analogs, is provided that employs a thiophosphorus compound, such as a thiophosphoric, dithiophosphoric, thiophosphinic, or dithiophosphinic acid disulfide or polysulfide, as a sulfurizing agent. The method of the invention may be used to sulfurize any phosphorous(III)containing intermediate. Preferably, the method is practiced on a commercial DNA synthesizer using phosophoramidite and/or phosphorthioamidite intermediates.
Claims5
A method of sulfurizing a phosphate or thiophosphite linkage in an oligonucleotide, the method comprising the step of reacting said phosphite or thiophosphite linkage with a thiophosphorus compound to form a phosphorothioate linkage or a phosphorodithioate linkage, respectively, wherein said thiophosphorus compound is selected from the group consisting of thiophosphoric acid disulfide, dithiophosphoric acid disulfide, thiophosphinic acid disulfide, and dithiophosphinic acid disulfide.
Dependencies are inferred from the claim text.