Enantioselective Rhodium(I)-Catalyzed [3+2] Annulations of Aromatic Ketimines Induced by Directed CH Activations
作者:Duc N. Tran、Nicolai Cramer
DOI:10.1002/anie.201105766
日期:2011.11.18
selectivity: Highly substituted indenylamines can be obtained with high enantioselectivity by formal [3+2] additions of aryl ketimines with internal alkynes. These rhodium(I)‐catalyzed processes proceed by selective CH activation of one of the two arene substituents, regioselective carbometalation of the alkyne, and enantioselective addition across the imine.
The invention pertains to heteroaromatic compounds that serve as effective phosphodiesterase (PDE) inhibitors. In particular, the invention relates to said compounds which are selective inhibitors of PDE10. The invention also relates to intermediates for preparation of said compounds; pharmaceutical compositions comprising said compounds; and the use of said compounds in a method for treating certain central nervous system (CNS) or other disorders.
syn-Selective Rhodium(I)-Catalyzed Allylations of Ketimines Proceeding through a Directed CH Activation/Allene Addition Sequence
作者:Duc N. Tran、Nicolai Cramer
DOI:10.1002/anie.201004179
日期:2010.10.25
On a Rh‐oll: Rhodium(I)‐catalyzed CH activations of ketimines and subsequent carborhodation of an allene led to an allyl metal species, which then allylated the imine directing group to give highly functionalized methylene dihydroindenyl amines (see scheme) with excellent regio‐ and diastereoselectivity.
Rhodium-Catalyzed Dynamic Kinetic Asymmetric Transformations of Racemic Allenes by the [3+2] Annulation of Aryl Ketimines
作者:Duc N. Tran、Nicolai Cramer
DOI:10.1002/anie.201304919
日期:2013.9.27
Racemization required: Rhodium(I)‐catalyzed CH activation directed by unprotected ketimines initiates selective [3+2] cycloaddition with allenes, providing access to highly substituted indenylamines. The reaction proceeds through the dynamic kinetic asymmetric transformation of racemic allenes. The catalyst controls the enantio‐ and diastereoselectivity, the regioselectivities of the CH activation and allene
The invention pertains to heteroaromatic compounds that serve as effective phosphodiesterase (PDE) inhibitors. In particular, the invention relates to said compounds which are selective inhibitors of PDE10. The invention also relates to intermediates for preparation of said compounds; pharmaceutical compositions comprising said compounds; and the use of said compounds in a method for treating certain central nervous system (CNS) or other disorders.