SYNTHESIS OF MORPHOLINO OLIGOMERS USING DOUBLY PROTECTED GUANINE MORPHOLINO SUBUNITS
申请人:REEVES MATTHEW DALE
公开号:US20090131624A1
公开(公告)日:2009-05-21
Morpholino compounds are provided having the structure:
where
R
1
is selected from the group consisting of lower alkyl, di(lower alkyl)amino, and phenyl;
R
2
is selected from the group consisting of lower alkyl, monocyclic arylmethyl, and monocyclic (aryloxy)methyl;
R
3
is selected from the group consisting of triarylmethyl and hydrogen; and
Y is selected from the group consisting of: a protected or unprotected hydroxyl or amino group; a chlorophosphoramidate group; and a phosphorodiamidate linkage to the ring nitrogen of a further morpholino compound or a morpholino oligomer. Such compounds include doubly protected morpholino guanine (MoG) monomers. Also described is their use in synthesis of morpholino oligomers.
Morpholino化合物具有以下结构:
其中
R1选自由较低烷基、二(较低烷基)氨基和苯基组成的群体;
R2选自由较低烷基、单环芳基甲基和单环(芳氧基)甲基组成的群体;
R3选自由三芳基甲基和氢原子组成的群体;以及
Y选自由受保护或未受保护的羟基或氨基团;氯磷酰胺基团;以及与另一种morpholino化合物或morpholino寡聚体的环氮原子形成磷酰二胺酸酯键的群体。这类化合物包括双保护的morpholino鸟嘌呤(MoG)单体。还描述了它们在morpholino寡聚体合成中的用途。