Sulfurizing reagents and their use for oligonucleotides...

C - Chemistry – Metallurgy – 07 – H

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C07H 21/04 (2006.01) C07C 311/03 (2006.01) C07D 207/48 (2006.01)

Patent

CA 2747999

An oligonucleotide which comprises at least one internucleotide linkage comprising a P-S-R bond and at least two nucleosides, wherein R corresponds to the formula (I) wherein A is a geminally substituted alkylene group, preferably CH2, X and Y are independently selected from S and O, and R0 is selected from the group consisting of optionally substituted carbon bonded organic residue, such as in particular optionally substituted alkyl or aryl, SRx, ORx and NRxRy wherein Rx and/or Ry are selected from H and organic residues and at least Rx is a substituent other than H. Another object of the invention is a sulfurizing agent useful for oligonucleotide manufacture and the manufacture thereof.

L'invention concerne un oligonucléotide qui comprend au moins une liaison internucléotidique comprenant une liaison P-S-R bond et au moins deux nucléosides, R correspondant à la formule (I) dans laquelle A représente un groupe alkylène à substitution géminale, de préférence CH2, X et Y sont indépendamment choisis parmi S et O, et R0 est choisi dans l'ensemble consistant en résidus organiques liés à un atome de carbone éventuellement substitués, comme, en particulier, les groupes alkyle ou aryle éventuellement substitués, SRx, ORx et NRxRy, dans lesquels Rx et/ou Ry sont choisis parmi H et des résidus organiques et au moins un Rx est un substituant autre que H. L'invention concerne également un agent de sulfurisation utile pour la fabrication de l'oligonucléotide, et sa fabrication.

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