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 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.
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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.
23 Citations
115 Claims
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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 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. - View Dependent Claims (2, 3, 4, 7, 8, 9, 10, 11, 12, 13, 16, 17, 18, 20, 22, 23, 24, 25, 26, 27, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 67, 69, 70, 71, 72, 73, 74, 75, 77, 78, 81, 82, 83, 84, 86, 87, 90, 92, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115)
- -OH moiety to form a condensed intermediate; and
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Specification