Suzuki cross-coupling of solid-supported chloropyrimidines with arylboronic acids.
The utility of the Suzuki cross-coupling to synthesize biaryl compounds is expanded herein to include reactions of resin-supported chloropyrimidines with boronic acids. In particular, an efficient method is described for the synthesis of a library of biaryl compounds from solid-supported chloropyrimidines. The Suzuki reaction was performed in an inert atmosphere using Pd(2)(dba)(3)/P(t-Bu)(3) as catalyst, spray-dried KF as base, and THF as solvent. The reaction was allowed to proceed overnight at 50 degrees C. Upon cleavage with acid, a library of 4-(substituted amino)-6-arylpyrimidines was obtained in moderate yield and high purity.
Wade
Janice V
JV
Discovery Partners International, Inc., ChemRx Division, 385 Oyster Point Blvd., Suite 1, South San Francisco, California 94080, USA.
Krueger
Clinton A
CA