Synthesis and selective cleavage of an oligodeoxynucleotide containing a bridged intemucleotide 5′-phosphorothioate linkage

Abstract
A self complementary oligodeoxynucleotide dodecamer containing an achiral bridged 5′-phosphorothloate linkage 3′-O-P-S-5′ has been prepared using the solid phase phosphoramidite procedure. For the incorporation of the phosphorothioate link we have used a 5′-(S-trityl)mercapto-5′-deoxythymidine-3′-phosphoramidlte. After coupling this building block the S-trityl group was removed by silver ions. The free thiol molety was then coupled with a standard phosphoramldite in the presence of tetrazole. After oxidation of the 5′-phosphorothioite with iodine/water the synthesis was continued with standard building blocks up to the desired dodecamer. This backbone modified dodecamer can be cleaved selectively and quantitatively at the P-S bond by silver or mercuric ions under very mild conditions.

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