Synthesis of backbone-modified morpholino oligonucleotides and chimeras using phosphoramidite chemistry

摘要

Amine-substituted morpholino oligonucleotides other than the classical N, N-dimethylamino PMO analogs and methods for efficiently synthesizing these oligonucleotides in high yield are provided. A morpholino oligonucleotide having a linker of thiophosphoramidate, phosphoramidate, phosphoramidate diester, and alkyl phosphoramidate. Chimeras can be made that include unmodified DNA / RNA and other analogs of DNA / RNA. These oligonucleotides form duplexes with complementary DNA or RNA that are more stable than natural DNA or DNA / RNA complexes, are active with RNase H1, and use standard lipid reagents. Can be transfected into cells. Accordingly, these analogs are useful for many applications. [Selection] Figure 4