IP Library Granted Patent US 10,144,747
Granted Patent B2
US 10,144,747 · App. 14/903,724 · Granted Dec 4, 2018

Reagents and methods for fluorinating a substrate

Inventor: David Vicic (Bethlehem, PA)
C07F3/06C07C17/263C07D215/18C07F15/04C07C2602/10
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Quick Facts
Patent No.
US 10,144,747
App. No.
14/903,724
Granted
Dec 4, 2018
Kind
B2
Abstract

Described herein are perfluoroalkylated zinc compounds having the structure of Formula (I) or Formula (II), which can be used to perfluoroalkylate organic, inorganic and organometallic substrates. Methods of making and using these compounds by reacting zinc or a dialkylzinc compound with a perfluoroalkyl dihalide in a solvent such as tetrahydrofuran, dioxane or diglyme, are also described.

Claims (31)

1. A compound of formula (I):

wherein:

n is an integer ranging from 2 to 6;

L is selected from one or more of tetrahydrofuran; dioxane; acetonitrile; diethyl ether; N-methylmorpholine; triethylamine; bipyridine; N,N,N′,N′-tetramethylethylenediamine; N,N,N′,N′-tetraethylethylenediamine; a glyme; or 1,3-dimethyl-3,4,5,6-tetrahydro-2(1H)pyrimidinone; and

m is an integer ranging from 1 to 3.

2. The compound of claim 1 , wherein n is 4.

3. The compound of claim 1 , wherein the glyme has the following formula: CH 3 O(CH 2 CH 2 O) t CH 3 ; wherein t is an integer between 1 and 10.

4. The compound of claim 1 , wherein the glyme is diethylene glycol dimethyl ether.

5. A method for preparing a compound of formula (I):

wherein:

n is an integer ranging from 2 to 6;

L is selected from one or more of tetrahydrofuran; dioxane; acetonitrile; diethyl ether; N-methylmorpholine; triethylamine; bipyridine; N,N,N′,N′-tetramethylethylenediamine; N,N,N′,N′-tetraethylethylenediamine; a glyme; or 1,3-dimethyl-3,4,5,6-tetrahydro-2(1H)pyrimidinone; and

m is an integer ranging from 1 to 3; the method comprising:

reacting a compound of Formula (III):

wherein v is an integer ranging from 2 to 6;

with a compound of Formula (IV):

Zn(R a ) 2   (IV)

in the presence of a solvent;

wherein:

each X is independently selected from Br; I; Cl; tosylate; mesylate; and CF 3 SO 3 − ; and

R a is C 1 -C 10 alkyl.

6. The method of claim 5 , wherein the solvent comprises a C 5 -C 8 alkyl compound.

7. The method of claim 5 , wherein the solvent comprises a hexane selected from n-hexane; 2-methylpentane; 3-methylpentane; 2,3-dimethylbutane; and 2,2-dimethylbutane.

8. A method of fluorinating a substrate comprising:

reacting a compound according to claim 1 with a halogenated nickel compound.

9. The method of claim 8 , wherein the halogenated nickel compound is NiBr 2.

10. A method of fluorinating a substrate comprising:

reacting a compound according to claim 1 with a halogenated heterocylic compound.

11. The method of claim 10 , wherein the heterocylic compound is a monocyclic or bicyclic 5-12 membered heterocyclic compound.

12. The method of claim 10 , wherein the heterocylic compound is selected from a pyrrolidine, a pyrole, a piperidine, a pyridine, an azepane, an azepine, an indole, a quinoline, a benzazepine, and a carbazole.

13. The method of claim 10 , wherein the halogenated heterocyclic compound is 2,3-diiodopyridine.

Assignments (1)
CONFIRMATORY LICENSE Recorded Apr 14, 2021
From: LEHIGH UNIVERSITY
To: UNITED STATES DEPARTMENT OF ENERGY
Reel/Frame 055926/0138 →
Continuity (2)
Provisional Application 61844067 · Jul 9, 2013
Related Publication 20160176901A1 · Jun 23, 2016