METHOD FOR THE SYNTHESIS OF PHOSPHORUS ATOM MODIFIED NUCLEIC ACIDS
First Claim
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1. A method for a synthesis of a nucleic acid comprising a chiral X-phosphonate moiety comprising:
- reacting a molecule comprising an achiral H-phosphonate moiety, a chiral reagent, and a nucleoside comprising a 5′
-OH moiety to form a condensed intermediate; and
converting the condensed intermediate to the nucleic acid comprising a chiral X-phosphonate moiety, wherein the nucleic acid comprises a modified sugar.
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Abstract
Described herein are methods of syntheses of phosphorous atom-modified nucleic acids comprising chiral X-phosphonate moieties. The methods described herein provide backbone-modified nucleic acids in high diasteteomeric purity via an asymmetric reaction of an achiral molecule comprising a chemically stable H-phophonate moiety with a nucleoside/nucleotide.
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Citations
19 Claims
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1. A method for a synthesis of a nucleic acid comprising a chiral X-phosphonate moiety comprising:
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reacting a molecule comprising an achiral H-phosphonate moiety, a chiral reagent, and a nucleoside comprising a 5′
-OH moiety to form a condensed intermediate; andconverting the condensed intermediate to the nucleic acid comprising a chiral X-phosphonate moiety, wherein the nucleic acid comprises a modified sugar. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19)
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Specification