Catalytic C(sp3)?H Arylation of Free Primary Amines with an exo Directing Group Generated In Situ
Herein, we report the palladium-catalyzed direct arylation of unactivated aliphatic C?H bonds in free primary amines. This method takes advantage of an exo-imine-type directing group (DG) that can be generated and removed in situ. A range of unprotected aliphatic amines are suitable substrates, undergoing site-selective arylation at the γ-position. Methyl as well as cyclic and acyclic methylene groups can be activated. Furthermore, when aniline-derived substrates were used, preliminary success with δ-C?H arylation was achieved. The feasibility of using the DG component in a catalytic fashion was also demonstrated.
Xu, Yan,Young, Michael C.,Wang, Chengpeng,Magness, David M.,Dong, Guangbin
supporting information
p. 9084 - 9087
(2016/07/26)
PYRROLOTRIAZINES AS ALK AND JAK2 INHIBITORS
The present invention provides a compound of formula (I) or a salt form thereof, wherein Q1, Q2, Q3, and Q4 are as defined herein. The compound of formula (I) has ALK and/or JAK2 inhibitory activity, and may be used to treat proliferative disorders.
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Page/Page column 455
(2010/08/05)
Palladium-catalyzed amidation of unactivated c(sp3)-h bonds: From anilines to indolines
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Neumann, Julia J.,Rakshit, Souvik,Droge, Thomas,Glorius, Frank
supporting information; experimental part
p. 6892 - 6895
(2009/12/26)
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