The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Jan. 02, 2018
Filed:
Mar. 17, 2015
Kaohsiung Medical University, Kaohsiung, TW;
Tzu-Pin Wang, Tainan, TW;
Yu-Chih Su, Tainan, TW;
KAOHSIUNG MEDICAL UNIVERSITY, , TW;
Abstract
The present invention discloses a method of harnessing versatile phosphoramidation reactions to regioselectively link a group of alkynyl-/azido-containing compounds to post-synthetic nucleic acids primed with phosphate at the 5' termini. The method includes steps of: (a) monophosphoramidating HN(CH)NHto the 5′ end of the nucleic acid to form an intermediate 1 where n is an integer from 2 to 6, and the intermediate 1 has a formula of: (b) amidating the free —NHgroup of the intermediate 1 with to form an intermediate 2; and (c) reacting the terminal —Ngroup of the intermediate 2 with 1-{3-{[4-(2-cyclooctyn-1-ylmethyl)benzoyl]amino}propyl}-4-{2-[4-(dimethylamino)phenyl]ethenyl}pyridinium hexafluorophosphate (Alkyne MegaStokes dye 608) by the SPAAC reaction to form modified nucleic acids. Without the presence of Cu(I), the modified nucleic acids were subjected to azide-alkyne cycloaddition in an aqueous solution to obtain various nucleic acid conjugates with a high yield.