IP Library Granted Patent US 8,889,857
Granted Patent B2
US 8,889,857 · App. 13/799,620 · Granted Nov 18, 2014

Phosphine-ligated palladium sulfonate palladacycles

Inventors: Nicholas C. Bruno (California, MD); Stephen L. Buchwald (Newton, MA)
Assignee: Massachusetts Institute of Technology
C07F15/006C07F9/28C07F15/0086C07B37/04
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Quick Facts
Patent No.
US 8,889,857
App. No.
13/799,620
Granted
Nov 18, 2014
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 (22)

1. A precatalyst of formula I:

wherein, independently for each occurrence,

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, phosphate, hydrogen phosphate, dihydrogen phosphate, phosphinate, and hypochlorite;

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

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

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 R 1 is H or alkyl.

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

wherein L is selected from the group consisting of PPh 3 , P(o-tol) 3 , PCy 3 , P(tBu) 3 , BINAP, dppf, dppp,

wherein L is selected from the group consisting of PPh 3 , P(o-tol) 3 , PCy 3 , P(tBu) 3 , BINAP, dppf, dppp,

wherein L is selected from the group consisting of

5. A dimer of formula IX:

wherein, independently for each occurrence,

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, phosphate, hydrogen phosphate, dihydrogen phosphate, phosphinate, and hypochlorite; and

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

6. The dimer of claim 5 , wherein R 1 is H or alkyl.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 7, 2013
From: BRUNO, NICHOLAS C.; BUCHWALD, STEPHEN L.
To: MASSACHUSETTS INSTITUTE OF TECHNOLOGY
Reel/Frame 030362/0883 →
CONFIRMATORY LICENSE Recorded May 3, 2013
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 030342/0360 →
Continuity (2)
Provisional Application 61657377 · Jun 8, 2012
Related Publication 20130331566A1 · Dec 12, 2013