申请人:MAZUR Wieslaw Adam
公开号:US20120071640A1
公开(公告)日:2012-03-22
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 CH
2
, X and Y are independently selected from S and O, and R
0
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. Other nucleotides described comprise at least one internucleotide linkage comprising a P—S—R bond, at least one internucleotide linkage comprising a P—S—R′ bond and at least three nucleosides wherein R′ is an organic residue other than the group R, preferably selected from a group consisting of an aryl group and a heteroaryl group which is bonded to the S-atom through an annular carbon atom.
该发明涉及一种寡核苷酸,其中至少包括一种由P-S-R键组成的核苷酸连接,以及至少两个核苷酸。其中,R对应于公式(I),其中A是一个双重取代的烷基,优选为CH2,X和Y分别选择自S和O,R0选择自一组由可选取代的碳键合有机残基组成,特别是可选取代的烷基或芳基,SRx、ORx和NRxRy,其中Rx和/或Ry选择自H和有机残基,至少Rx是除H之外的取代基。该发明的另一个目的是用于寡核苷酸制备的硫化剂及其制备方法。其他核苷酸至少包括一种由P-S-R键组成的核苷酸连接,至少包括一种由P-S-R'键组成的核苷酸连接,以及至少三个核苷酸,其中R'是除R之外的有机残基,优选选择自一个芳基和一个杂环芳基,该芳基或杂环芳基通过环状碳原子与S原子键合。