IP Library Granted Patent US 9,481,645
Granted Patent B2
US 9,481,645 · App. 14/627,360 · Granted Nov 1, 2016

Composition, synthesis, and use of a new class of isonitriles

Inventors: Fraser Fergusson Fleming (Falls Church, VA); Jesus Armando Lujan-Montelongo (Tlalnepantla de Baz, MX)
Assignee: Duquesne University of the Holy Ghost
C07C323/26C07C249/02C07C323/25C07C2101/08C07C2101/14
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Quick Facts
Patent No.
US 9,481,645
App. No.
14/627,360
Granted
Nov 1, 2016
Kind
B2
Abstract

This invention relates to novel isonitriles, including arylthio isonitriles, and methods for their preparation. The isonitriles include a conjugated ring system. The structure is designed with the flexibility to have multiple substitution patterns. The isonitriles may be used in applications including, but not limited to, pharmaceutical compositions.

Claims (20)

1. An isonitrile compound of a structure of Formula I:

wherein, X is selected from oxygen and sulfur, R 1 is selected from alkyl and aryl, R 2 is selected from hydrogen and XR 1 , R 3 is selected from hydrogen and XR 1 , and R 4 is selected from alkyl and an aromatic or non-aromatic, cyclic or polycyclic structure, or

wherein, X is selected from oxygen and sulfur, R 1 is selected from alkyl and aryl, R 2 and R 3 form a benzo ring, and R 4 is selected from alkyl and an aromatic or non-aromatic, cyclic or polycyclic structure.

2. The compound of claim 1 , wherein R 4 is selected from alkyl and a cyclic six-membered ring.

3. The compound of claim 1 , wherein R 1 is selected from C 1 -C 6 alkyl and aryl.

4. The compound of claim 1 , wherein R 1 is selected from C 1 -C 4 alkyl and aryl.

5. The compound of claim 1 , wherein said compound has a structure of Formula II:

wherein X, R 1 , R 2 , and R 3 are as defined for Formula I.

6. The compound of claim 1 , wherein said compound has a structure of Formula III:

wherein X, R 1 , R 2 , and R 3 are as defined for Formula I.

7. An isonitrile compound of a structure of Formula IV:

wherein X is selected from oxygen and sulfur, R 1 is selected from alkyl and aryl, R 2 is selected from hydrogen and XR 1 , and R 4 is selected from alkyl and an aromatic or non-aromatic, cyclic or polycyclic structure.

8. A method of preparing an isonitrile comprising:

reacting a compound of a structure of Formula III:

wherein, X is selected from oxygen, sulfur and nitrogen, R 1 is selected from alkyl and aryl, R 2 is selected from hydrogen and XR 1 , R 3 is selected from hydrogen and XR 1 ,

with an electrophile in an exchange reaction to form compounds represented by general structures of Formulas V or VI:

wherein, R 5 is C 1 -C 4 alkyl.

9. The method of claim 8 , wherein the electrophile is selected from the group consisting of diphenyl disulfide, methyl iodide, propyl bromide, propylene oxide, cyclohexanone, propyl iodide, cyclohexenone, and mixtures thereof.

10. The method of claim 8 , wherein R 1 is selected from C 1 -C 6 alkyl and aryl.

11. The method of claim 8 , wherein R 1 is selected from C 1 -C 4 alkyl and aryl.

Assignments (2)
CONFIRMATORY LICENSE Recorded Jun 15, 2015
From: DUQUESNE UNIVERSITY
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 035909/0128 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 20, 2015
From: FLEMING, FRASER FERGUSSON; LUJAN-MONTELONGO, JESUS ARMANDO
To: DUQUESNE UNIVERSITY OF THE HOLY GHOST
Reel/Frame 034994/0628 →
Continuity (2)
Provisional Application 61942843 · Feb 21, 2014
Related Publication 20150239835A1 · Aug 27, 2015