Method of synthesizing sulfurized oligonucleotide analogs
First Claim
1. 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.
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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.
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Citations
5 Claims
- 1. 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.
Specification