Phosphotriester oligonucleotides, amidities and method of prepar

Organic compounds -- part of the class 532-570 series – Organic compounds – Carbohydrates or derivatives

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536 221, 536 253, 536 2531, 536 2532, 536 2533, 536 2534, 536 2671, 536 2672, 536 2674, 536 268, C07H 1906, C07H 1916, C07H 2100

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061244457

ABSTRACT:
Oligonucleotides having bioreversible phosphate blocking groups can be used as pro drugs for the oligonucleotides. The bio-reversible blocking groups can be removed by intercellular enzymes, particularly carboxyesterases, to provide the unprotected oligonucleotide. The oligonucleotides can be prepared via post synthesis alkylation reactions or utilizing amidite type chemistry wherein the bioreversible phosphorus protecting group is formed as an integral part of the amidite reagent.

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