IP Library Granted Patent US 8,981,086
Granted Patent B2
US 8,981,086 · App. 14/521,727 · Granted Mar 17, 2015

Phosphine-ligated palladium sulfonate palladacycles

Inventors: Nicholas C. Bruno (California, MD); Stephen L. Buchwald (Newton, MA)
Assignee: Massachusetts Institute of Technology
C07F15/006
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Quick Facts
Patent No.
US 8,981,086
App. No.
14/521,727
Granted
Mar 17, 2015
Kind
B2
Abstract

Described are palladium precatalysts, and methods of making and using them. The palladium precatalysts show improved stability and improved reactivity in comparison to previously-described palladium precatalysts.

Claims (29)

1. A precatalyst of formula III:

wherein, independently for each occurrence,

X is a non-coordinating anion;

R 1 is H, alkyl, haloalkyl, hydroxy, alkoxy, aryloxy, aryl, or halo;

L is a trialkylphosphine, triarylphosphine, dialkylarylphosphine, alkyldiarylphosphine, bis(phosphine), phosphoramide, amine, bis(amine), or N-heterocyclic carbene; and

R 2 is alkyl, haloalkyl or aryl.

2. The precatalyst of claim 1 , wherein L is selected from the group consisting of PPh 3 , Ph 2 P—CH 3 , PhP(CH 3 ) 2 , P(o-tol) 3 , PCy 3 , P(tBu) 3 , BINAP, dppb, dppe, dppf, dppp,

R x is alkyl, aralkyl, cycloalkyl, or aryl;

X 1 is CH or N;

R 3 is H or alkyl;

R 4 is H, alkoxy, or alkyl;

R 5 is alkyl or aryl; and

n is 1, 2, 3, or 4.

3. The precatalyst of claim 1 , wherein X is selected from the group consisting of boron tetrafluoride, tetraarylborates, hexafluoroantimonate, phosphorus tetrafluoride, phosphorus hexafluoride, alkylsulfonate, haloalkylsulfonate, arylsulfonate, perchlorate, bis(alkylsulfonyl)amide, bis(fluoroalkylsulfonyl)amide, bis(arylsulfonyl)amide, (fluoroalkylsulfonyl)(fluoroalkylcarbonyl)amide, nitrate, nitrite, sulfate, hydrogensulfate, alkyl sulfate, aryl sulfate, carbonate, bicarbonate, carboxylate, phosphate, hydrogen phosphate, dihydrogen phosphate, phosphinate, and hypochlorite.

4. The precatalyst of claim 1 , wherein R 1 is H or alkyl.

5. The precatalyst of claim 1 , wherein R 2 , where present, is substituted or unsubstituted alkyl.

6. The precatalyst of claim 1 , wherein R 2 , where present, is substituted or unsubstituted aryl.

7. The precatalyst of claim 1 , wherein the precatalyst is selected from the group consisting of:

wherein R is H, alkyl, or aryl; L is selected from the group consisting of PPh 3 , Ph 2 P—CH 3 , PhP(CH 3 ) 2 , P(o-tol) 3 , PCy 3 , P(tBu) 3 , BINAP, dppb, dppe, dppf, dppp,

R x is alkyl, aralkyl, cycloalkyl, or aryl; X 1 is CH or N; R 3 is H or alkyl; R 4 is H, alkoxy, or alkyl; R 5 is alkyl or aryl; and n is 1, 2, 3, or 4.

8. A dimer of:

wherein, independently for each occurrence,

X is a non coordinating anion; and

R 1 is H, alkyl, haloalkyl, hydroxy, alkoxy, aryloxy, aryl, or halo;

R 2 is alkyl, haloalkyl or aryl.

9. The dimer of claim 8 , wherein X is selected from the group consisting of boron tetrafluoride, tetraarylborates, hexafluoroantimonate, phosphorus tetrafluoride, phosphorus hexafluoride, alkylsulfonate, haloalkylsulfonate, arylsulfonate, perchlorate, bis(alkylsulfonyl)amide, bis(fluoroalkylsulfonyl)amide, bis(arylsulfonyl)amide, (fluoroalkylsulfonyl)(fluoroalkylcarbonyl)amide, nitrate, nitrite, sulfate, hydrogensulfate, alkyl sulfate, aryl sulfate, carbonate, bicarbonate, carboxylate, phosphate, hydrogen phosphate, dihydrogen phosphate, phosphinate, and hypochlorite.

10. The dimer of claim 8 , wherein R 1 is H or alkyl.

11. The dimer of claim 8 , wherein R 2 , where present, is substituted or unsubstituted alkyl.

12. The dimer of claim 8 , wherein R 2 , where present, is substituted aryl or unsubstituted aryl.

Assignments (2)
CONFIRMATORY LICENSE Recorded Jun 7, 2018
From: MASSACHUSETTS INSTITUTE OF TECHNOLOGY
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 046313/0289 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 12, 2014
From: BRUNO, NICHOLAS C.; BUCHWALD, STPEHEN L.
To: MASSACHUSETTS INSTITUTE OF TECHNOLOGY
Reel/Frame 034152/0160 →
Continuity (3)
Division 13799620 · Mar 13, 2013
Provisional Application 61657377 · Jun 8, 2012
Related Publication 20150045570A1 · Feb 12, 2015