IN SITU PREPARATION OF NUCLEOSIDE PHOSPHORAMIDITES AND OLIGONUCLEOTIDE SYNTHESIS

摘要

The invention provides novel bifunctional phosphitylating reagents and theirapplication in in situ preparation of 5'-protected nucleosidephosphoramidites and synthesis of oligonucleotides. Bifunctionalphosphitylating reagents according to the invention react quickly withnucleosides under neutral or weakly basic conditions, without an additionalactivation step. In addition, the bifunctional phosphitylatingreagents according to the invention generate chemoselectively thecorresponding nucleoside phosphoramidites in situ, without need to purifythe nucleoside phosphoramidites before using them in oligonucleotidesynthesis. Finally, the bifunctional phosphitylating reagents accordingto the invention are relatively stable and easy to handle.