| 摘要 |
New methods of synthesizing mono- and oligo- nucleotide H-phosphonates are disclosed. The methods comprise contacting a mononucleoside with phosphonic acid and benzoyl anhydride to yield the corresponding mononucleoside H-phosphonate. Preferably, a catalytic amount of triphosgene is also used. A similar procedure can be used to couple a first mononucleoside to a second mononucleoside or to an oligonucleotide, the method comprising contacting, in the presence of benzoic anhydride and, preferably, a catalytic amount of triphosgene, a mononucleotide or oligonucleotide having a free 5'hydroxyl with a mononucleoside having a 3'hydroxyl-bearing phosphorous moiety (preferably H-phosphonate).
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