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Beilstein J. Org. Chem. 2012, 8, 1804–1813, doi:10.3762/bjoc.8.206
Graphical Abstract
Scheme 1: Three-step sequence for the preparation of γ-lactams from maleimides, aldehydes and amines. Potenti...
Scheme 2: The transfer of the diastereoselective ratio of 3 to the enantioselectivity of the overall process ...
Scheme 3: Combination of the Michael addition step with the reductive amination/lactamization step and of the...
Scheme 4: Combination of the Michael addition, the reductive amination/lactamization, and the epimerization s...
Scheme 5: Chemspeed 4 × 8 × 8 library of γ-lactams 6.
Beilstein J. Org. Chem. 2012, 8, 1200–1207, doi:10.3762/bjoc.8.133
Figure 1: Representative biologically active aminomethylcoumarins.
Scheme 1: Approach to diversely substituted coumarins.
Scheme 2: Scope of the decarboxylative coupling.
Scheme 3: Scope of Suzuki-coupling of coumarinyl acetates.
Scheme 4: Coupling of (coumarinyl)methyl acetates with N- and S-nucleophiles.
Scheme 5: Scope of the coumarinyl acetate and aryl sulfinate coupling reaction.
Scheme 6: Scope of the coumarinyl acetate and amine coupling reaction.
Figure 2: Library planning for amine (A) and coumarin (C) coupling partners.
Figure 3: Results for the synthesis of a 128-member library of aminated coumarins by using the Chemspeed SLT1...