Solid phase synthesis of oligonucleotide N3'-P5' phosphoramidate

Details Solid phase synthesis of oligonucleotide N3'-P5' phosphoramidate Solid phase synthesis of oligonucleotide N3'-P5' phosphoramidate

1996-06-14

1998-10-20

Kunz, Gary L.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carbohydrates or derivatives

536 253, 536 2533, C07H 100, C07H 102

Patent

active

058247939

ABSTRACT:
The invention provides a method of synthesizing oligonucleotide N3'.fwdarw.P5' phosphoramidates using an amine-exchange reaction of phosphoramidites in which a deprotected 3'-amino group of a solid phase supported oligonucleotide chain is exhanged for the amino portion of a 5'-phosphoramidite of an incoming monomer which has a protected 3'-amino group. The resulting internucleotide phosphoramidite linkage is then oxidized to form a stable protected phosphoramidate linkage. The method of the invention greatly improves product yields and reduces reagent usage over currently available methods for synthesizing the above class of compound.

REFERENCES:
patent: 5476925 (1995-12-01), Letsinger et al.
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