期刊
CHEMISTRY-A EUROPEAN JOURNAL
卷 14, 期 8, 页码 2443-2452出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.200701621
关键词
amination; anilines; asymmetric catalysis; carbenes; palladium
Pd-N-heterocyclic carbene (NHC)-catalyzed Buchwald-Hartwig amination protocols mediated by Pd-PEPPSI precatalysts is described. These protocols provide access to a range of hindered and functionalized drug-like aryl amines in high yield with both electron-deficient and electron-rich aryl- and heteroaryl chlorides and bromides. Variations in solvent polarity, base and temperature are tolerated, enhancing the scope and utility of this protocol. A mechanistic rationalization for base strength (pK(b)) requirements is also provided.
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