Patent · US Active

Synthesis of 2′,3′— and 3′,5′—cyclic phosphate mono-and oligonucleotides

US8618279B2 · kind B2 · utility

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9Claims
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Assignee

Inventors

Key dates

Filing dateJan 15, 2010
Grant dateDec 31, 2013
Priority date
Expiry dateApr 2, 2032

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07H19/213
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

The invention provides a novel method for the chemical synthesis of 2′,3′-cyclic phosphate and phosphorothioate of mono and terminated oligonucleotides synthesis. The invention also provides a novel method of for the chemical synthesis of 2′,3′- and 3′,5′-cyclic phosphate and phosphorothioate mononucleotide nucleotides. The process is based on quick and efficient cyclization of phosphoramidate moiety and neighboring hydroxyl group. The present invention is directed towards the synthesis of high purity DNA and RNAs, specifically to introduce cyclic phosphate at 3′-end of oligonucleotides. Such DNA and RNA's have extensive application in therapeutics, diagnostics, drug design, and selective inhibition of an RNA sequence within cellular environment, in pre-tRNA cleavage and in ribozyme ligation. The 2′,3′-cyclic phosphate nucleosides are involved in a vast number of applications in molecular biology in general and mammalian cells in particular. The invention also envisions providing kits comprising at least one composition disclosed in the present invention.

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