Efficient guanidination of the phosphate linkage towards cationic phosphoramidate oligonucleotides
Résumé
An efficient postsynthesis method of guanidination of oligonucleotides was employed to introduce several guanidinium groups into internucleotide phosphoramidate linkages. The amino functions of aminobutylphosphoramidate links were converted to guanidine butylphosphoramidates using a solution of O-methylisourea hemisulfate in aqueous ammonia, in a short reaction time. The synthesis of various fully guanidylated oligonucleotides was successfully performed to provide a new class of cationic phosphoramidate oligonucleotides.
An efficient postsynthesis method of guanidination of oligonucleotides was employed to introduce several guanidinium groups into internucleotide phosphoramidate linkages in order to obtain a new class of cationic oligonucleotides.
Domaines
Chimie thérapeutique
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Tetrahedron Letters 2003 Vol. 44 Issue 35 Pages 6579-6582.pdf (180.19 Ko)
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