title: Rapid HATU-mediated solution phase siRNA conjugation.
abstract: 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.
authors: Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., Inc., West Point, Pennsylvania 19486, United States. jeffrey_aaronson@merck.com
authors: Jeffrey G
authors: JG
authors: Aaronson
authors: Lee J
authors: LJ
authors: Klein
authors: Aaron A
authors: AA
authors: Momose
authors: Ann M
authors: AM
authors: O'Brien
authors: Anthony W
authors: AW
authors: Shaw
authors: Thomas J
authors: TJ
authors: Tucker
authors: Yu
authors: Y
authors: Yuan
authors: David M
authors: DM
authors: Tellers
mesh_terms: D000577:Amides / Q000138:chemical synthesis; D000588:Amines / Q000737:chemistry; D002264:Carboxylic Acids / Q000737:chemistry; D003432:Cross-Linking Reagents / Q000737:chemistry*; D008722:Methods; D034741:RNA, Small Interfering / Q000737:chemistry*; D012996:Solutions
chemical_list: D000577:Amides; D000588:Amines; D002264:Carboxylic Acids; D003432:Cross-Linking Reagents; D034741:RNA, Small Interfering; D012996:Solutions