B1 Non-refereed article in a scientific journal
Biodegradable phosphate protections of oligonucleotides
Authors: Poijarvi P, Lonnberg H
Publication year: 2005
Journal: Collection Symposium Series
Journal name in source: Chemistry of Nucleic Acid Components
Journal acronym: COLL SYMPOS SERIES
Volume: 7
First page : 457
Last page: 459
Number of pages: 3
ISBN: 80-86241-25-4
Abstract
Oligonucleotides bearing biodegradable phosphate protecting groups have been synthesized on a solid support. For this purpose, two dimeric building blocks, viz. (5'-O-(4,4'-dimethoxytrityl) (R-p,S-p)-O-P-[2,2-bis-(ethoxycarbonyl)-3-(pivaloyl-oxypropyl)]-P-thiothymidylyl-(3',5')thymidine 3'-[O-(2-cyanoethyl)-(N,N-diisopropyl)phosphoramidite] (1) and 5'-O-(4,4'-dimethoxytrityl) (R-p,S-p)-O-P-{[2-cyano-2-(2-phenyl-ethyl)-aminocarbonyl]-3-(pivaloyloxy)propyl)thymidylyl(3',5')-thymidine 3'-(H-phosphonate)} (2), were prepared. Enzymatic deprotection of the oligonucleotide prodrugs has been studied.
Oligonucleotides bearing biodegradable phosphate protecting groups have been synthesized on a solid support. For this purpose, two dimeric building blocks, viz. (5'-O-(4,4'-dimethoxytrityl) (R-p,S-p)-O-P-[2,2-bis-(ethoxycarbonyl)-3-(pivaloyl-oxypropyl)]-P-thiothymidylyl-(3',5')thymidine 3'-[O-(2-cyanoethyl)-(N,N-diisopropyl)phosphoramidite] (1) and 5'-O-(4,4'-dimethoxytrityl) (R-p,S-p)-O-P-{[2-cyano-2-(2-phenyl-ethyl)-aminocarbonyl]-3-(pivaloyloxy)propyl)thymidylyl(3',5')-thymidine 3'-(H-phosphonate)} (2), were prepared. Enzymatic deprotection of the oligonucleotide prodrugs has been studied.
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