A series of squaramide-based organocatalysts were facilely synthesized and applied as hydrogen bonding organocatalysts in the enantioselective Michael addition of nitroalkanes to chalcones. These organocatalysts promoted the Michael addition with low catalyst loading under high temperature (80 °C), affording the desired R or S enantiomers of the products flexibly in high yields with excellent enantioselectivities (93-96% ee) by the appropriate choice of organocatalysts.
At present the only FDA-approved therapy for Alzheimer's disease involves the administration of acetylcholinesterase inhibitors, to alleviate the cholinergic deficit associated with this disease. However, none of the approved drugs is ideal in efficacy or tolerability. One possible strategy to improve selectivity and potency is to design drugs that can simultaneously bind to the catalytic and peripheral anionic sites of AChE. In this review we will describe the development of dimeric AChE inhibitors, from the early observations of high inhibition potency by bis-quaternary inhibitors, to the structure-based design of dimers based on tacrine, huperzine A, galanthamine, and polyamines.
As an important class of heterocyclic scaffolds, 2‐imidazolines have attracted the attention from the chemists interested in natural products, pharmaceutical chemistry, synthetic organic chemistry, coordination chemistry, and homogeneous catalysis. To fulfill the demand of structural diversity, many efficient methods towards 2‐imidazolines, as well as modifications of traditional methods, have been reported in the past two decades. 2‐Imidazolines have been developed as ligands in homogeneous catalysis, for the substitution on the nitrogen atom that provides an opportunity for fine‐tuning of the electronic effect. This review summarizes recent advances in the synthesis of 2‐imidazolines and their applications in homogeneous catalysis.
In Table 3 of this Communication, the chemical structures of the substituents of products 8 q and 8 r were inadvertently switched. The correct entries are shown here. In Table 4, the structures of the major isomers 12 a and 12 c were printed incorrectly. The correct structures are shown here. The editorial office apologizes for these oversights. Table 3: Catalytic asymmetric hydrogenation of quinoline derivatives. [a] Entry R Product Yield [%] ee [%] Config 17 8 q > 99 [c] 90 R 18 8 r > 99 [c] 95 R
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