Compositions and methods for the synthesis of oligonucleotides h

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

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536 28, 536 29, C07H 1900

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active

050719742

ABSTRACT:
Methods for the chemical 5' phosphorylation of oligonucleotides. An embodiment of the present invention includes reacting the 5' terminus of an oligonucleotide with a composition represented by the formula: ##STR1## wherein if Y and Z are taken separately, each represent an alkyl, aryl, arylalkyl, cycloalkyl or cycloalkylaryl; or if Y and Z are taken together, Y and Z form an alkyl or alkylene chain with both terminal valence bonds of said chain being attached to the nitrogen atom to which Y and Z are attached; or if Y and Z are taken together, with the nitrogen atom, Y and Z form a nitrogen heterocycle including at least one additional heteroatom selected from the group consisting of nitrogen, oxygen, and sulfur. W and X are selected from the group of functional groups subject to nucleophilic attack or .beta.-elimination and are removed.

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patent: 4500707 (1985-02-01), Caruthers et al.
patent: 4757141 (1988-06-01), Fung et al.
patent: 4762779 (1989-08-01), Snitman
Smith et al., Nucleic Acids Research, 13, 2399-2412 (1985).
McBride et al., Tetrahedron Letters, 24, 245-248 (1983).
Beaucage et al., Tetrahedron Letters, 22, 1859-1862 (1981).

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