Joseph M Fox

US Patent:

6888029, May 3, 2005

Filed:

Jan 22, 2003

Appl. No.:

10/349198

Inventors:

Stephen L. Buchwald - Newton MA, US
Joseph M. Fox - Wilmington DE, US

Assignee:

Massachusetts Institute of Technology - Cambridge MA

International Classification:

C07C209/08
C07C209/10
C07C209/22

US Classification:

564396, 564405, 564406, 564413

Abstract:

The present invention relates to a process for the preparation of N-aryl amine and N-aryl amide compounds. Generally, the process of the present invention involves reacting a compound having a primary or secondary amino or amido group with an arylating compound, in the presence of a weak base and a transition metal catalyst, under reaction conditions effective to form an N-aryl amine or N-aryl amide compound, the transition metal catalyst comprising a Group 8 metal, e. g. , Ni, Pd, or Pt, and at least one carbene-containing ligand. Typically, the transition metal catalyst is formed in a preceding step from the conjugate acid form of the carbene ligand, a stoichiometric amount of a strong base, and a Group 8 metal atom or ion.