A highly regioselective amination of 6-aryl-2,4-dichloropyrimidine.
[reaction: see text]. A highly regioselective amination of 6-aryl-2,4-dichloropyrimidine with aliphatic secondary amines and aromatic amines has been developed which strongly favors the formation of the C4-substituted product. The reactions with aliphatic amines are carried out using LiHMDS as the base and are catalyzed by Pd, while the aromatic amines require no catalyst.
Peng
Zhi-Hui
ZH
Department of Process Research, Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065, USA. zhihui_peng@merck.com
Journet
Michel
M
Humphrey
Guy
G