A highly regioselective amination of 6-aryl-2,4-dichloropyrimidine |
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Authors: | Peng Zhi-Hui Journet Michel Humphrey Guy |
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Institution: | Department of Process Research, Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065, USA. zhihui_peng@merck.com |
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Abstract: | 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. |
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