IP Library Granted Patent US 8,940,859
Granted Patent B2
US 8,940,859 · App. 13/418,676 · Granted Jan 27, 2015

Alkynes and methods of reacting alkynes with 1,3-dipole-functional compounds

Inventors: Geert-Jan Boons (Athens, GA); Jun Guo (Athens, GA); Xinghai Ning (Athens, GA); Margaretha Wolfert (Athens, GA)
Assignee: University of Georgia Research Foundation, Inc.
C07D495/04A61K47/48853A61K49/0021A61K49/0043A61K49/0052C07C35/37C07C49/683C07C211/42C07C251/44C07D249/16C07D261/20C07D271/12C07D307/94C07D311/90C07C2103/36
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Quick Facts
Patent No.
US 8,940,859
App. No.
13/418,676
Granted
Jan 27, 2015
Kind
B2
Abstract

1,3-Dipole-functional compounds (e.g., azide functional compounds) can be reacted with certain alkynes in a cyclization reaction to form heterocyclic compounds. Useful alkynes (e.g., strained, cyclic alkynes) and methods of making such alkynes are also disclosed. The reaction of 1,3-dipole-functional compounds with alkynes can be used for a wide variety of applications including the immobilization of biomolecules on a substrate.

Claims (25)

1. A dibenzocyclooctyne having the formula:

wherein:

each R 1 and R 2 is hydrogen;

X represents CHOR 3 ; and

R 3 represents an organic group comprising a biotin fragment.

2. A dibenzocyclooctyne having the formula:

wherein:

each R 1 and R 2 is hydrogen;

X represents CHOR 3 ; and

R 3 represents an organic group comprising a covalently bound organic dye.

3. A dibenzocyclooctyne having the formula:

wherein:

each R 1 is independently selected from the group consisting of hydrogen, halogen, hydroxy, alkoxy, nitrate, nitrite, sulfate, and a C1-C10 organic group;

each R 2 is independently selected from the group consisting of hydrogen, halogen, hydroxy, alkoxy, nitrate, nitrite, sulfate, and a C1-C10 organic group;

X represents C═N—OR 3 , C═N—NR 3 R 4 , CHOR 3 , or CHNHR 3 ;

R 3 represents an organic group attached to a nanoparticle; and

R 4 represents hydrogen or an organic group.

4. A method of preparing a heterocyclic compound, the method comprising:

combining at least one azide-functional compound with at least one dibenzocyclooctyne according to claim 3 ; and

allowing the at least one azide-functional compound and the at least one alkyne to react under conditions effective to form the heterocyclic compound.

5. An alkyne of the formula:

wherein:

each R 1 and R 2 is hydrogen;

X represents CHOR 3 ; and

R 3 represents an organic group.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 18, 2015
From: BOONS, GEERT-JAN; GUO, JUN; NING, XINGHAI; WOLFERT, MARGARETHA
To: UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC.
Reel/Frame 036347/0977 →
Continuity (6)
Continuation 12743632
Provisional Application 61004021 · Nov 21, 2007
Provisional Application 61007674 · Dec 14, 2007
Provisional Application 61137061 · Jul 25, 2008
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