Rapid HATU-Mediated Solution Phase siRNA Conjugation

Conditions for facile solution-phase amide conjugation of amine-modified siRNA with a diverse set of carboxylic acid partners using the coupling reagent HATU are described. These conditions eliminate the need for isolated activated esters and allow for rapid access to conjugates with a wide range of...

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Veröffentlicht in:	Bioconjugate chemistry 2011-08, Vol.22 (8), p.1723-1728
Hauptverfasser:	Aaronson, Jeffrey G, Klein, Lee J, Momose, Aaron A, O’Brien, Ann M, Shaw, Anthony W, Tucker, Thomas J, Yuan, Yu, Tellers, David M
Format:	Artikel
Sprache:	eng
Schlagworte:	Amides - chemical synthesis Amines - chemistry Carboxylic Acids - chemistry Chemical compounds Chemical reactions Cross-Linking Reagents - chemistry Methods Ribonucleic acid RNA RNA, Small Interfering - chemistry Solution chemistry Solutions
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Beschreibung
Zusammenfassung:	Conditions for facile solution-phase amide conjugation of amine-modified siRNA with a diverse set of carboxylic acid partners using the coupling reagent HATU are described. These conditions eliminate the need for isolated activated esters and allow for rapid access to conjugates with a wide range of lipophilicity and functionality in good yield.
ISSN:	1043-1802 1520-4812
DOI:	10.1021/bc2001227